MEDISunday, 10 September 2006

7:00 PM-9:00 PM Moscone Center -- Hall D, Poster
General Poster Session
Sponsored by Eli Lilly
Organizer:David P. Rotella
Ceramide and its inhibitor: Syntheses and applications
Shang-U Kim, Shehzad H. Ayub, Robin Polt
Synthetic approaches for Fumonisin B1 and B2
Shang-U Kim, Shehzad H. Ayub, Robin Polt
Suggested biosynthetic pathway of tunicate-derived benzopolysulfanes
David Aebisher, Edyta M. Brzostowska, Mahendran Adaickpillai, Alexander Greer
Synthesis of tritiated CT-100, a small molecule inhibitor of microtuble formation, for use in determining binding kinetics
Brianne S. Raccor, Charitha Madiraju, Raghavan Balachandran, Pui Kai Li, Billy W. Day
Synthesis of fluorinated tetraphenylporphyrins for potential use in photodynamic therapy
Kip Conner, Valentina Tan, Meden Isaac, Ursula Simonis
Design of glutathione transferase-activated nitric oxide-releasing prodrugs as anticancer agents
Thomas C. Wilde, Brett M. Showalter, Joseph E. Saavedra, Paul J. Shami, Kenneth D. Tew, Danyelle M. Townsend, Xinhua Ji, Larry K. Keefer
Synthesis of Nordihydroguaiaretic analogs and their anti-cancer properties
Joseph E. Blecha, Jennifer Chow, Marc O. Anderson, Jack Youngren, Clifford E. Berkman
Prenyl monophosphate prodrugs as Farnesyltransferase and Geranylgeranyltransferase I inhibitors
Michelle Maynor, Michelle Clark, Sarah A. Reigard, Richard F. Borch, Richard A. Gibbs
Resveratrol analogs as therapeutics for cancer
Justin J. Heynekamp, Lorraine M. Deck, Lucy A. Hunsaker, David L. Vander Jagt
Synthesis and singlet oxygen generation of hydroxy-branched porphyrins for potential photosensitizers
Ke Feng, Xiu R. Bu
Dual-targeting taxoid anticancer drug conjugates
Stanislav Jaracz, Iwao Ojima
DNA cleavage chemistry of pyridine-based heterocyclic skipped aza-enediynes: Deoxyribosyl hydrogen atom abstraction and guanine oxidation
Bodin Tuesuwan, Sean M. Kerwin
Discovery and development of benzocyclohexene, -heptene and –octene compounds as potential vascular disrupting agents
Madhavi Sriram, Nathan Grohmann, John Hall, Kevin G. Pinney
Altering the substrate specificity of the Baeyer-Villiger type monooxygenase mtmOIV to produce new analogs of the anticancer agent Mithramycin
Miranda Beam, Jürgen Rohr
Structure-activity relationship study and in vivo evaluation of a potent and specific peptidomimetic ligand of alpha4 beta1 integrin
Ruiwu Liu, Li Peng, Mirela Andrei, Greg W. Bocash, Kit S. Lam
G-quadruplex binding agents: 4-Hydroxybenzo(h)quinoline derivatives
Jennifer. Baltz, Hanumantharao Paritala
Studies of Echinacea on HeLa and MCF-7 cancer cell lines
Jeremy Jensen, Fathi T. Halaweish
Discovery of potent indole and indolizine derivatives displaying cytotoxicity against multidrug resistant cancer cell lines
David James, Keizo Koya, Hao Li, Shoujun Chen, Zhiqiang Xia, Weiwen Ying, Yaming Wu, Lijun Sun
The sigma-2 selective tropane analog RHM-138 induces apoptosis In EMT-6 breast cancer cells
Justin Rothfuss, Chenbo Zeng, Suwanna Vangveravong, Wenhua Chu, Zhude Tu, Richard Hotchkiss, Katherine C. Chang, Robert H Mach
Applications of RNAi against cancer-associated genes
Scott E. Martin, Tamara L. Jones, Natasha J. Caplen
Synthesis, metal binding, and cytotoxicity of UK-1 analogs
Mireya L. Rodriguez, Sean M. Kerwin
Pro-drugs of ARQ 501: Designs suitable for other carbonyl-containing drugs and candidates
Jean-Marc Lapierre, Manish Tandon, Yanbin Liu, Hui Wu, E. Kelleher, Dasharatha Reddy, Yinglin Han, Steve Couture, Sapna Makhija, Zhiwei Jiang, Mark A. Ashwell
Targeted delivery of ARQ 501 to tumors using novel chemical linking strategies
Manish Tandon, Jean-Marc Lapierre, Yanbin Liu, Hui Wu, Erika Volckova, Sapna Makhija, Ron Savage, Zhiwei Jiang, Ying Si, Mark A. Ashwell
Chemical synthesis of C-2 taxoids and their tubulin binding abilities and antitumor activities
Chun-Gang Yang, Ruth Matesanz, Ana Alcaraz, Lei Wang, Xuan Li, Isabel Barasoain, Ronghua Liu, Frances J. Sharom, James P. Snyder, J. Fernando Díaz, Wei-Shuo Fang
Discovery and pre-clinical development of a novel inhibitor of oncogenic B-Raf
Prabha N. Ibrahim, Jiazhong Zhang, Hanna Cho, Shumeye Mamo, Ryan Bremer, Samuel Gillette, Abhinav Kumar, Daniel Fong, Weiru Wang, Yong-Liang Zhu, Adhirai Marimuthu, Yoshihisa Suzuki, Billy Lam, Julie Rice, James Tsai, Calvin Settachatgul, Rafe Shelloe, John Cantwell, Brain West, Ben Powell, Gaston Habets, Chao Zhang, D. Rick Artis, Peter Hirth, Gideon Bollag
Synthesis and biological evaluation of pancratistatin analogs with the truncated cyclitol portion of the molecule
Madhuri Manpai, Alexander Kornienko
Successful delivery of siRNA to human chronic myelogenous leukemia cells by cobalamin-mediated endocytosis
Randy Y. Adachi, Charles B. Grissom
Synthesis and biological evaluation of heterocyclic analogs of podophyllotoxin
Madhuri Manpadi, Alexander Kornienko, Elena Rozhkova, Igor V. Magedov
Characterization of the “R” binding site of P-glycoprotein: Using novel chalcogenoxanthylium tetramethylrosamine analogs for the stimulation of ATPase activity
Michael K. Gannon II, Gregory Tombline, David J Donnelly, Jason J. Holt, Youngjae You, Mao Ye, Cara L. Nygren, Michael R. Detty
Development of a novel carbohydrate microarray and its application in cancer diagnostics and therapeutics
Joseph C. Manimala, Tim Roach, Zhitao Li, Jeffrey C. Gildersleeve
Synthesis of asymmetric, heavy chalcogen tetramethylrosamine derivatives: Micromolar inhibition at the “R” site of P-Glycoprotein
Jason J. Holt, Gregory Tombline, Michael R. Detty
PDT efficiency of pheophorbide a analogs upon conjugating with cyclo(RGDfK)
Suresh K. Pandey, Shipra Dubey, Xiang Zheng, Yihui Chen, Carrie A. Batt, Janet Morgan, Michael J. Ciesielski, Munnawar Sajjad, Hani A. Nabi, Robert A. Fenstermaker, Allan R. Oseroff, Ravindra K. Pandey
Design and synthesis of a folate receptor-targeted chemotherapeutics: Folic acid conjugate of desacetylvinblastine hydrazide (EC 145)
Iontcho R. Vlahov, Hari Krishna R. Santhapuram, Paul J. Kleindl, Stephen J. Howard, Katheryn M. Stanford, Christopher P. Leamon
Synthesis of 1-/2-substituted-[1, 2, 3]triazolo[4, 5-g]phthalazine-4, 9-diones and evaluation of their cytotoxicity and DNA topoisomerase inhibitory activity
Hee-Kyung Rhee, Hyen Joo Park, Sang Kook Lee, Chong-Ock Lee, Hea-Young Park Choo
Tetracyclic pyrazoles, open analogs and derivatives: From 7-Chloro-1,4,5,10-tetrahydro-1,2,10-triaza-cyclopenta[a]fluorene to three new scaffolds
Daniela Berta, Simona Bindi, Alexander Cameron, Giovanni Cervi, Daniele Fancelli, Ronald D Ferguson, Barbara Forte, Sergio Mantegani, Maria Menichincheri, Maurizio Pulici, Ermes Vanotti, Mario Varasi, Paola Vianello, Fulvia Roletto, Aurelio Marsiglio
Design, synthesis and evaluation of novel compounds for use in the prodrug approach to cancer chemotherapy
Gavin D. Couch, Christopher J. Moody
Design and synthesis of ring-fused and conformationally restrained epothilone analogs
Weiqiang Zhan, Yi Jiang, Susan Bane, Abhijit Banerjee, Dennis C. Liotta, James P. Snyder
EPR and molecular modeling studies of spin-labeled DNA antisense agents
Robyn R. Ayscue, Peter M. Gannett
Synthesis, cytotoxicity, and DNA topoisomerase inhibitory activity of benzonaphthofurandione and benzofuroquinolinedione derivatives
Hee-Kyung Rhee, Hyen Joo Park, Sang Kook Lee, Chong-Ock Lee, Hea-Young Park Choo
Synthesis and cytotoxic activity of 1-En-3-one lupane triterpenoids
Ali Koohang, Ze-Qi Xu, Erika L. Szotek, Nathan D. Majewski, Aye Aye Mar, David A. Eiznhamer, Michael T. Flavin
Novel human lipoxygenases inhibitors discovered using virtual screening with homology models
Victor A. Kenyon, Ilya Chorny, Wendy J. Carvajal, Theodore R. Holman, Matthew P. Jacobson
Structure activity relationship studies of flavonoids as potent inhibitors against 12-hLO, 15-hLO and 15-hLO-2
Rachana V. Ohri, Vasquez-Martinez Yesseny, Silvia Sepúlved-Boza, Theodore Holman
pH-Sensitive biotinylated dendritic MRI probe to improve detection of liver tumors
Md. Meser Ali, Mark D. Pagel
Chemical genetics approach to breast cancer therapy
Kedra C Cyrus, Yang-eon Kim, Kyung-Bo Kim
Design, synthesis, and evaluation of novel bimodal ligands for radioimmunotherapy of cancer
Hyun-Soon Chong, Thien Le, Phuong Bui, Noah Birch, Xiang Wang, Katherine Hammes
Fluorous-phase synthesis of minor groove binding agents related to distamycin
Jennifer. Baltz, Sreeman K. Mamidyala
Synthesis of the carcinogenic C8–carboxyphenyl & C8–hydroxymethylphenyl guanine adducts and their effect on DNA conformation
Vorasit Vongsutilers, Peter M. Gannett
Optimizing lead anologs for activated a4b1 integrin
Richard D. Carpenter, Mark J. Kurth, Kit S. Lam
Synthesis and bioevaluation of novel theophylline-dendrimer conjugates
Xingyi Yang, Minghui Chai, Ping Zhou, Shengxiang Qiu
Design, synthesis and testing of novel styryl benzyl sulfones as potent anti-cancer agents
Muralidhar R Mallireddigari, Venkat R Pallela, Stephen C Cosenza, Stanley C Bell, Balaiah Akula, Vinaykumar Billa, Revathi Patti, E. Premkumar Reddy, MV. Ramana Reddy
Synthesis and cytotoxic evaluation of novel thiazolo[5,4-b]quinoline derivatives
Alfonso Lira-Rocha, Susana Vázquez-Olvera, Marco A. Loza-Mejía, Angelina Quintero, José D. Solano, Adriana Camacho, Sergio Molina
Antiproliferative effect of select plant extracts on different cancer cells
Ipek Goktepe, Norma Sneed, Bonita Milford, Mohamed Ahmedna
Evaluation of efficient intracellular release of anticancer agents from tumor-targeting delivery system
Shuyi Chen, Xianrui Zhao, Jin Chen, Iwao Ojima
First 3D pharmacophore modeling of androgen receptor down-regulating agents (ARDAs): Discovery of potent anti-prostate cancer agents
Vincent C. O. Njar, Puranik Purushottamachar, Aakanksha Khandelwal, Neha Maheshwari, Pankaj Chopra, Lalji K. Gediya
Phosphoramidate derivatives of hydroxy steroids as inhibitors of prostate-specific membrane antigen
Lisa Yong Wu, Helen Page, Yoko Toriyabe, Marc O. Anderson, Clifford E. Berkman
Small α-helix mimetics for the inhibition of the estrogen receptor-coactivator interaction
Jorge Becerril, Andrew D. Hamilton
Novel vitamin D receptor (VDR) and androgen receptor (AR) ligands with diphenylmethane skeleton
Shinnosuke Hosoda, Aya Tanatani, Ken-ichi Wakabayashi, Kazuo Nagasawa, Hiroyuki Miyachi, Yuichi Hashimoto
New 3-beta-halopropionyloxi-4,16-pregnadiene-6,20-dione derivatives as 5-alpha-reductase inhibitors
Eugene A. Bratoeff
Novel non-steroidal/non-anilide type androgen antagonists effective toward mutated androgen receptor
Aya Tanatani, Ken-ichi Wakabayashi, Hiroyuki Miyachi, Yuichi Hashimoto
Novel retinoid antagonists bearing trifluoromethyl groups
Hiroyuki Kagechika, Michimasa Maeda, Tomoya Hirano, Emiko Kawachi, Yuichi Hashimoto
Novel C-17-heteroaryl steroids as potential inhibitors of CYP17
Vincent C. O. Njar, Jorge A. R. Salvador, Vânia M. A. Moreira, Tadas Sean Vasaitis
Synthesis and activities of imidazolyl derivatives as novel farnesyltransferase inhibitors
Yeelana Shen, Philip G. Kasprzyk, Gregoire Prevost, Jesse Z. Dong
SAR studies of potent antitumor agent FR901464
Brian J. Albert, Nancy L. Czaicki, Kazunori Koide
Synthesis and cytotoxicity of Sansalvamide A derivatives in drug resistant colon cancers
Katerina Otrubova, Po-Shen Pan, Thomas J. Styers, Ahmet Kekec, Rodrigo Rodriguez, Joseph D. Brown, Stephanie Lapera, Suchitra Ravula, Erin Singh, Chung-Mao Pan, Emily Parry, Crystal Sanchez, Shelli R. McAlpine, Kathleen L. McGuire
Small molecule apoptosis inducer in multiple myeloma cell lines
Ramzi Ayyad, Kaapjoo Park, Derek C. Cole, Joseph R. Stock, Jun Xu, Chao-Pei Betty Chang, Wenshan Hao
Function oriented synthesis: Design, synthesis, and biological evaluation of novel chemotherapeutic agents in the bryolog series
Paul A. Wender, Jeremy L. Baryza, Joshua C. Horan, Vishal A. Verma
Ligands for the TRP-M8 receptor found in prostate cancer cells
Lok Him Yu, Chi Ching Joyce Leung, Xiaoliu Guo, Ahamindra Jain
Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents for p21 deficient cells: Structure activity relationships of analogs with amide modifications
Fuk-Wah Sum, Lijing Chen, Lane Wooder, Eric Honores, Daniel Wang, Dennis Powell, Miriam Miranda, Sridhar Rabindran
A novel duocarmycin-analog based pro-drug, Delivered as an antibody drug conjugate for targeted cancer therapy
Liang Chen, Sanjeev Gangwar, Chin Pan, Chetana Rao, Bilal Sufi, Sharon Boyd, Mary Huber, Peter Sattari, Mary Do, Rory Dai, Colin Chong, Carol Soderberg, Hao Li, Haichun Huang, Haibin Chen, Lynae Green, Janette Sung, David Passmore, Vangipuram Rangan, Vincent Guerlavais, Killian Horgan, Nik Sharkov, Krista Heaton, Tom Kempe, Mohan Srinivasan, Shrikant Deshpande, Pina Cardarelli, David J. King
Characterizing binding interactions of the PH1 domain of AFAP-110: A precursor to anticancer therapeutic design
John E Jett, Daniel C Flynn, Henry G Zot, Peter M. Gannett
Discovery of potent small molecule inhibitors of the MDM2-p53 interaction through pharmacophore-based and structure-based database screening
Yipin Lu, Zaneta Nilolovska-Coleska, Su Qiu, Sanjeev Kumar, Wei Gao, Xueliang Fang, Dongguang Qin, Shaomeng Wang
MDM2 inhibitory peptides: Side chains cyclization as a method of stabilization of the biologically active helical conformation
Krzysztof Krajewski, Zaneta Nikolovska-Coleska, Shaomeng Wang, Peter P. Roller
Design, synthesis and evaluation of spirooxindoles as potent and specific non-peptide small-molecule inhibitors of the MDM2-p53 interaction
Dongguang Qin, Ke Ding, Guoping Wang, Zaneta Nikolovska-Coleska, Yipin Lu, Su Qiu, Sanjeev Kumar, Wei Gao, Jeanne Stuckey, Krzysztof Krajewski, Peter Roller, Shaomeng Wang
Apoptotic pathway induced by HA 14-1, a small-molecule antagonist for Bcl-2 protein
Chengguo Xing, Jignesh M Doshi, Defeng Tian, Sadiya N Addo
Pharmacophore- and structure-based approaches to the development of small molecule inhibitors for Bcl-2 family proteins and MAP kinases
Xiyun Zhang, Michele F. Rega, Jui-Wen Huang, John Stebbins, Barbara Becattini, Maurizio Pellecchia
Design, synthesis and evaluation of a new class of potent and cell-permeable small molecule inhibitors of Bcl-2 and Mcl-1
Guozhi Tang, Ke Ding, Jie Guo, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Renxiao Wang, Jianting Long, Su Qiu, Sanjeev Kumar, Wei Gao, Jeanne Stuckey, Krzysztof Krajewski, Sheng Jiang, Peter P. Roller, Shaomeng Wang
Structure-based discovery of small molecule inhibitors of XIAP
Yipin Lu, Zaneta Nilolovska-Coleska, Su Qiu, Shaomeng Wang
Theoretical design of a novel series of enediynes containing metal center
Edyta M. Brzostowska, Roald Hoffmann
Indenopyrazoles: Potent, broad-spectrum cyclin dependent kinase inhibitors
Christopher J. Oalmann, Nick Bockovich, Maureen Caligiuri, Faith Kaplan, Jianxing Huang, Arthur Kluge, Lou Lamphere, Mohamud Mohamud, Judson Richard, Ram Siya, Katya Tsaioun, Shaoshan Wang, Zhonggou Wang
Discovery of PF-371989: A novel Tie2 kinase inhibitor
Susan LaGreca, Joel T. Arcari, Gary Borzillo, Michael J Chen, Tracey Clark, Bruce Cohen, Marcus Ewing, William M. Hungerford, Catherine Soderstrom, Shefali Kakar, Aaron Kanter, Lissie Knauth, Yong Lu, Luis Martinez-Alsina, Matthew A Marx, Nandini Patel, Carl Thompson, Norma Tom, Matt Wessel, Patrick W Vincent
Synthetic approaches to novel analogs of Tie-2 kinase inhibitors
Joel T. Arcari, Michael J Chen, William Hungerford, Nandini Patel, Matthew A Marx, Susan LaGreca, Luis Martinez-Alsina, Matthew Wessel, Stephen Anderson, Jon Bordner, Gary Borzillo, Tracey Clark, Bruce Cohen, Marcus Ewing, Catherine Soderstrom, Shefali Kakar, Aaron Kanter, Lissie Knauth, Carl Thompson, Norma Tom, Ivan Samardjiev, Patrick W Vincent
Design and synthesis of selective Tie-2 inhibitors
Nandini Patel, Joel T. Arcari, Gary Borzillo, Michael J Chen, Tracey Clark, Bruce Cohen, Marcus Ewing, William M. Hungerford, Shefali Kakar, Aaron Kanter, Lissie Knauth, Susan LaGreca, Yong Lu, Luis Martinez-Alsina, Matthew A Marx, Catherine Soderstrom, Carl Thompson, Norma Tom, Matt Wessel
Synthesis, structure-activity relationships, and mechanism of action of novel indirubin derivatives as potent anti-proliferative agents with CDK2 inhibitory activities
Yong-Chul Kim, Isak Im, Soo Jung Choi, Eun Sil Lee, Sang Kook Lee
Discovery and optimization of potent ACK1 inhibitors – Part I: 4-Amino substitution is important for potency improvement
Jinqian Liu, Rajiv Sharma, Sarah Lively, Simon Burkitt, Andrew Clase, Chris Farthing, XianYun Jiao, David Kopecky, Frank Kayser, Stephen Shuttleworth, Martin Harrison, Paul Faulder, Shyun Li, Holger Wesche, Rommel Mallari, Ellyn Farrelly, Shou-Hua Xiao, Jinsong Liu, Zhulun Wang, Juan Jaen
Discovery and optimization of potent ACK1 inhibitors – Part II: Structural modification of the furanopyrimidine core
David Kopecky, Simon Burkitt, Andrew Clase, Ellyn Farelli, Chris Farthing, Paul Faulder, David Frenkel, Martin Harrison, Juan Jaen, XianYun Jiao, Frank Kayser, Shyun Li, Jinqian Liu, Jinsong Liu, Sarah Lively, Rajiv Sharma, Astrid Strelow, Edward van der Horst, Zhulun Wang, Holger Wesche, Shou-Hua Xiao
Discovery and optimization of potent ACK1 inhibitors – Part III: Selected 4-amino substitution affords very potent inhibitors
Sarah Lively, Simon Burkitt, Mario Cardozo, Andrew Clase, Ellyn Farelli, Chris Farthing, Paul Faulder, Martin Harrison, Juan Jaen, XianYun Jiao, Frank Kayser, David Kopecky, Shyun Li, Jinqian Liu, Jinsong Liu, Rommel Mallari, Rajiv Sharma, Astrid Strelow, Edward van der Horst, Zhulun Wang, Holger Wesche, Shou-Hua Xiao
A new binding mode for inhibitors in Src reminiscent of Gleevec in Abl
Joel Renick, Andrew McPherson, Kathy Barrett, Jianguo Cao, Richard Fine, Colleen Gritzen, John Hood, Xinshan Kang, Chi-Ching Mak, Glenn Noronha, Ved P. Pathak, Richard Soll, Ute Splittgerber, Binqi Zeng
Validation of novel binding interaction for tyrosine kinases via crystal structures of low nM Src inhibitors: Implications for structure based drug design
Ved P. Pathak, Andrew McPherson, Kathy Barrett, Jianguo Cao, Richard Fine, Colleen Gritzen, John Hood, Xinshan Kang, Boris Klebansky, Dan Lohse, Chi-Ching Mak, Ismail Moarefi, Glenn Noronha, Joel Renick, Richard Soll, Ute Splittgerber, Binqi Zeng, Hong Zhu
Synthesis of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives and investigation of their roles against human protein kinase CK2
Sureyya Olgen, Claudia Götz, Joachim Jose
Synthesis and characterization of 2,4-diaryl-2,5-dihydropyrrole-2-(3'phenol) inhibitors of the mitotic kinesin KSP
Robert M. Garbaccio, Edward S. Tasber, Mark E. Fraley, George D. Hartman, Robert B. Lobell, Carolyn A. Buser, Weikang Tao, Hans E. Huber, Nancy E. Kohl, Youwei Yan, Lawrence C. Kuo, Maricel Torrent, Thomayant Prueksaritanont, Cathy Shu, Donald Slaughter
Synthesis and biological evaluation of (3Z)-3-quinolin-2(1H)-ylidene-1,3- dihydro-2H-indol-2-one derivatives as novel vascular endothelial growth factor-2 tyrosine kinase inhibitors
Kiyohiro Samizu, Hiroyuki Hisamichi, Akira Matsuhisa, Itsuro Shimada, Takanori Koike, Isao Kinoyama, Masahiko Hayakawa, Shunichiro Matsumoto, Nobuaki Taniguchi, Kiyoshi Yahiro, Naoko Katayama, Yukitaka Ideyama, Mayumi Yamano, Sadao Kuromitsu, Katsunori Tajinda, Nobuaki Amino, Minoru Okada, Makoto Takeuchi, Mitsuaki Ohta
Synthesis and SAR of cyanoguanidine and nitroethylene containing thiophene carboxamides as c-Kit inhibitors
Bijoy Panicker, Andrew Crew, Mark Bittner, Linda Castaldo, Arlindo Castelhano, Andrew Cooke, Dong Hanqing, Andrew Garton, Jennifer Kahler, An-Hu Li, Li Qiu, Alun Smith, Lawrence Tardibono, Qinghua Weng, Tao Zhang
3-Amino benzo[d]isoxazoles as novel multitargeted receptor tyrosine kinase inhibitors
Zhiqin Ji, Asma A. Ahmed, Daniel H. Albert, Jennifer J. Bouska, Peter F. Bousquet, George A. Cunha, Keith B. Glaser, Eric F. Johnson, Jun Guo, Junling Li, Patrick A Marcotte, Maria D. Moskey, Lori J. Pease, Nirupama B. Soni, Kent D. Stewart, Paul Tapang, Melinda S. Yates, Steven K. Davidsen, Michael R. Michaelides
SAR of 3-(1H-Benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of IGF-1R Kinase: Balancing oral exposure and Cyp inhibition
Xiaopeng Sang, Kurt Zimmermann, Mark D. Wittman, Mark G. Saulnier, Upender Velaparthi, David Langley, David B. Frennesson, Peiying Liu, Joan Carboni, Aixin Li, Ann Greer, Zheng Yang, Praveen Balimane, Dolatrai M. Vyas
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors: Design, synthesis and biological activity
Damian O. Arnaiz, Judi Bryant, Yuo-Ling Chou, Paul M. Hrvatin, Imadul Islam, Monica J. Kochanny, Wheeseong Lee, Gary B. Phillips, Hongyi Yu, Marc Adler, Marc Whitlow, Dao Lentz, Mark A. Polokoff, James M. Wu, Daguang Zhu, Richard I. Feldman
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors: Optimization of BX-517
Imadul Islam, Damian O. Arnaiz, Greg Brown, Judi Bryant, Yuo-Ling Chou, Paul M. Hrvatin, Monica J. Kochanny, Wheeseong Lee, Gary B. Phillips, Hongyi Yu, Shendong Yuan, Marc Adler, Marc Whitlow, Dao Lentz, Mark A. Polokoff, James M. Wu, Jun Shen, Janette Walters, Elena Ho, Babu Subramanyam, Sandra L. Biroc, Bruno Alicke, Daguang Zhu, Richard I. Feldman
Thieno[3,2-c]pyrazoles a new class of Aurora inhibitors
Paola Vianello, Simona Bindi, Daniela Berta, Alexander Cameron, Matteo D'Anello, Barbara Forte, Valeria Pittalà, Mario Varasi, Juergen Moll, Fulvia Roletto, Patrizia Carpinelli, Paola Storici, Paolo Cappella, Daniele Fancelli
Design and synthesis of target kinase inhibitor library
Q. John Yu, Faming Zhang
Influence of novel heterocyclic sidechains on the SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridin-2-one inhibitors of the IGF-1R kinase
David B. Frennesson, Mark G. Saulnier, Charles Struzynski, David Langley, Upender Velaparthi, Peiying Liu, Kurt Zimmermann, Xiaopeng Sang, Francis Y. Lee, Joan Carboni, Aixin Li, Ann Greer, Praveen Balimane, Zheng Yang, Chiehying Chang, John Sack, George L. Trainor, Mark D. Wittman, Dolatrai M. Vyas, Ricardo Attar, Marco Gottardis
Src inhibitors with sub nM VEGFR2 activity: Discovery and SAR
Elena Dneprovskaia, Andrew McPherson, Kathy Barrett, Jianguo Cao, Richard Fine, Colleen Gritzen, John Hood, Xinshan Kang, Chi-Ching Mak, Glenn Noronha, Ved P. Pathak, Joel Renick, Richard Soll, Binqi Zeng
Synthesis and SAR of novel inhibitors of the MLK family
Matthew Curry, Thelma S. Angeles, George Gessner, Diane E. Gingrich, Robert L. Hudkins, Jean Husten, Teresa O'Kane, Bethann McKenna, Allison Zulli
Design, synthesis and structure activity relationship within a series of 4-amino-thienopyridines, dual KDR/FGFR tyrosine kinase inhibitors
Y. Chen, K. Luk, T Flynn, L. McDermott, Omar Morales, P. Rossman, M. Simcox, S-S. So, P Wovkulich, H. Yang, Z. Zhang
Design and synthesis of potent small-molecule inhibitors of Stat-3
Jianyong Chen, Zaneta Nikolovska-Coleska, Cindy Gomez, Chao-Yie Yang, Wei Gao, Krzysztof Krajewski, Sheng Jiang, Peter Roller, Shaomeng Wang
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one based potent, and selective Chk-1 inhibitors
Le Wang, Gerard M. Sullivan, Laura Hexamer, Lisa A. Hasvold, Reema Thalji, Magdalena Przytulinska, Zhi-Fu Tao, Gaoquan Li, Zehan Chen, Zhan Xiao, Wen-Zhen Gu, John Xue, Mai-Ha Hui, Philip Metra, Peter Kovar, Haiying Zhang, Chang Park, Kent Stewart, Hing L. Sham, Thomas Sowin, Saul Rosenberg, Nan-Horng Lin
Discovery of tricyclic pyrazoles as potent checkpoint-1 kinase inhibitors
Yunsong Tong, Akiyo Claiborne, Zhi-Fu Tao, Peter Kovar, Chang Park, Zehan Chen, R. Bruce Credo, Kent D. Stewart, Haiying Zhang, Saul Rosenberg, Hing L. Sham, Thomas Sowin, Nan-Horng Lin
Development of substituted indolylindazoles as potent and selective Chek1 kinase inhibitors
Justin T. Steen, Mark E. Fraley, Edward Brnardic, George D. Hartman, Youwei Yan, Sanjieev Munshi, Mari Ikuta, Lawrence C. Kuo, Constantine Kreatsoulas, Michael Reilly, Elizabeth Mahan, Steve Stirdivant, Bob Drakas, Eileen Walsh, Kelly Hamilton, Carolyn Buser, Keith Rickert, Weikang Tao, James Hardwick, Xianzhi Mao, Steve Beck, Robert B. Lobell, Laura Sepp-Lorenzino
Structure-based design, synthesis and biological evaluation of macrocyclic Chk1 Inhibitors
Zhi-Fu Tao, Le Wang, Yunsong Tong, Gaoquan Li, Magdalena Przytulinska, Gerard Sullivan, Zehan Chen, Zhan Xiao, Wendy Gu, John Xue, Mai-Ha Bui, Philip Merta, Peter Kovar, Haiying Zhang, Chang Park, Kent D. Stewart, Hing L. Sham, Thomas Sowin, Saul H. Rosenberg, Nan-Horng Lin
Development of substituted indolylquinolinones as potent Chek1 kinase inhibitors
Shaei Huang, Rob Garbaccio, Mark Fraley, Justin T. Steen, George Hartman, Youwei Yan, Sanjieev Munshi, Mari Ikuta, Lawrence Kuo, Constantine Kreatsoulas, Michael Reilly, Elizabeth Mahan, Steve Stirdivant, Bob Drakas, Eileen Walsh, Kelly Hamilton, Carolyn Buser, Keith Rickert, Weikang Tao, James Hardwick, Xianzhi Mao, Steve Beck, Rob Lobell, Laura Sepp-Lorenzino
Novel thieno[3,2-b]pyridine scaffold based inhibitors of the c-Met and VEGFR receptor family
Stephen Claridge, Franck Raeppel, Marie-Claude Granger, Naomy Bernstein, Oscar Saavedra, Lijie Zhan, David Llewellyn, Amal Wahhab, Robert Déziel, Gabi Rahil, Normand Beaulieu, Hannah Nguyen, Isabelle Dupont, Annie Barsalou, Carole Beaulieu, Ian Chute, Serge Gravel, Marie-France Robert, Sylvain Lefebvre, Marja Dubay, James Wang, Jeffrey Besterman, A. Robert Macleod, Arkadii Vaisburg
4-Phenyl-6H-2,6-diaza-as-indacene-1,3-dione inhibitors of the G2/M DNA damage checkpoint kinase Wee1
R. John Booth, Derek J. Sheehan, Daniel F. Ortwine, Peter L. Toogood, Alexander J. Bridges, William A. Denny, K Hook, Alan J Kraker, Ho Lee, Brian D Palmer, John Quin III, Chris Squire
Probing the ATP-binding site of heat shock protein 90 (Hsp90) with synthetic macrolactones: Synthesis of simple analogs of radicicol as potent Hsp90 inhibitors
Nicolas Proisy, Christopher J. Moody
Structure-activity relationships of small molecule inhibitors of Hsp90
M. Kyle Hadden, Stephanie A. Hill, Steven M. Schebler, Robert L. Matts, Brian S. J. Blagg
Structure-activity relationship studies of libraries of potent Hsp90 inhibitors
Yung-tzung Huang, Brian Blagg
Paper Withdrawn
Hsp90 inhibitors: A study of coumarin antibiotic derivatives
Donna J. Lubbers, Joseph A. Burlison, Brian S. J. Blagg
Novobiocin analogs: Development and evaluation of novel small molecule Hsp90 inhibitors
Joseph A. Burlison, Donna J. Lubbers, Brian S. J. Blagg
2, 4-Diamino-6-arylthino[2,3-d]pyrimidines as potential dihydrofolate reductase inhibitors
Aleem Gangjee, Xilin Zhou, Roy L. Kisliuk, Sherry F. Queener
Novel 5-substituted, 2,4-diaminofuro[2,3-d]pyrimidines as potential multi-receptor tyrosine kinases and dihydrofolate reductase inhibitors in single molecules
Aleem Gangjee, Lu Lin, Michael Ihnat, Linda A. Warnke, Jessica E. Thorpe, Roy L. Kisliuk
Non-classical 5-aryl-furo[2,3-d]pyrimidines and 6-aryl-pyrrolo[2,3-d]pyrimidines as potential dihydrofolate reductase and/or thymidylate synthase inhibitors
Aleem Gangjee, Hiteshkumar D. Jain, Sherry F. Queener, Roy L. Kisliuk
Design, synthesis, and evaluation of novel 5-substituted, 2,4-diaminofuro[2,3-d]pyrimidines as single agent multireceptor tyrosine kinase and dihydrofolate reductase inhibitors
Aleem Gangjee, Wei Li, Michael A Ihnat, Linda A. Warnke, Jesssica E. Thorpe, Roy L. Kisliuk
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance
Aleem Gangjee, Jianming Yu, Staci N. Keller, Charles D. Smith
Synthesis of classical diamino furo[2,3-d] pyrimidine analogs as antifolates
Aleem Gangjee, Lei Wang, Larry H. Matherly, Yijun Deng
Polyaminohydroxamic acids and polyaminobenzamides the selectively inhibit histone deacetylase 6
Sheeba Varghese, Amy Hacker, Tracey Murray-Stewart, Robert A. Casero, Patrick M. Woster
Heterobiaryl hydroxamic acids as potent inhibitors of histone deacetylase (HDAC) possessing significant anti-proliferative cellular activity
David E. Clark, Steve Price
Synthesis and SAR of N-hydroxy-1,2-disubstituted-1H-benzoimidazol-5-yl-acrylamides as a novel class of histone deacetylase inhibitors
Haishan Wang, Niefang Yu, Hongyan Song, Dizhong Chen, Weiping Deng, Pek Ling Lye, Yong Zou, Melvin Ng, Joyce Chang, Eric T Sun, Kanda Sangthongpitag, Xukun Wang, Xiaofeng Wu, Hwee Hoon Khng, Siok Kun Goh, Pauline Yeo, Xin Liu, Evelyn Goh, Lee Sun New, Kantharaj Ethirajulu, Michael Entzeroth
Design and synthesis of arylamino-(2-aminophenyl)-benzamides or cinnamides (A) and heteroaryl -N-(2-aminophenyl)-benzamides (B) as a novel class of histone deacetylase inhibitors
Nancy Zhihong Zhou, Oscar Moradei, Stéphane Raeppel, Silvana Leit, Sylvie Frechette, Frédéric Gaudette, Isabelle Paquin, Giliane Bouchain, Naomy Bernstein, Franck Raeppel, Oscar Saavedra, Soon Hyung Woo, Arkadii Vaisburg, Marielle Fournel, Ann Kalita, Aihua Lu, Marie-Claude Trachy-Bourget, Pu T. Yan, Jianhong Liu, Zuomei Li, Gabi Rahil, A. Robert Macleod, James Wang, Jeffrey Besterman, Daniel Delorme
Synthesis and evaluation of cyclopeptide inhibitors of histone deacetylase
Charles M Marson, Stephane Sengmany, Brian Middleton, Jonathan Dines, N Shaun B Thomas
The computational search for novel histone deacetylase class I isozymes
Emilio Xavier Esposito, Gregory R. Cook
Design and synthesis of histone deacetylase 6 selective inhibitors
Takayoshi Suzuki, Akiyasu Kouketsu, Yukihiro Itoh, Shinya Hisakawa, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata
Discovery of second generation farnesyl protein transferase inhibitors
Hugh Y. Zhu, Alan B. Cooper, Jagdish Desai, Ronald J. Doll, V. Girijavallabhan, Dinanath Rane, James Wang, Paul Kirschmeier, Ming Liu, W. Robert Bishop, Robert Patton, Linda James, Corey Strickland, Amin Nomeir
Alternative route to compound 1: Utilization of an alpha-ketone arylation/oxidation, SNAr and Ullman reaction: An alternative route to Compound 1
Joel Robert Calvin
Glycorandomization of colchicine influences cytotoxicity and mechanism of action
Aqeel Ahmed, Noël, R Peters, Megan, K Fitzgerald, Jon S. Thorson
Evaluating bed stability of a new axial compression packing technology to traditional slurry packed columns for high throughput HPLC preparative purifications
Peter C Rahn, Tivadar Farcas, Gareth Friedlander, Joshua Heng, Emmet Welch
Synthesis of 5-nitroimidazole derivatives of tert-butyl ester of aminoacids
Iwona E. Weidlich, Stanislaw Sobiak
Paper Withdrawn
Synthesis and evaluation of Estradiol-PEG-DNA alkylation agents using click chemistry
Edward Y. Hua, David C. Labaree, Richard B. Hochberg, Robert N. Hanson
Series of novel polysulfide diketopiperazines produced by the fungus Fusarium merismoides
Hui Y. Yang, Haiyin He, John Hucul, Debbie Roll, Xidong Feng, Wenshan Hao, Jun Xu
Substrate activity screening (SAS): A fragment-based method for the rapid identification of nonpeptidic protease inhibitors
Andrew W. Patterson, Warren J. L. Wood, Jonathan A. Ellman
Soluble guanylyl cyclase activation by a series of aryl disulfanyl dinitrates
Adrian C. Nicolescu, Gregory R. J. Thatcher, Brian M. Bennett
Design, synthesis, and biochemical evaluation of ribitylaminopyrimidine substrate analogs of lumazine synthase as potential enzyme inhibitors and mechanistic probes
Arindam Talukdar, Adelbert Bacher, Markus Fisher, Boris Illarionov, Mark Cushman
Polyamine functionalized SPE polymers: Effective tools for reaction work-up
Paul A Boguszewski, Alasdair A MacDonald, Aubrey J Mendonca, Frank P Warner
Reactivity, selectivity and compatibility: A practical review of polymer supported coupling reagents
Paul A Boguszewski, Alasdair A MacDonald, Aubrey J Mendonca, Frank P Warner
Structure-activity relationship studies on cyclic peptide-based CXCR4 antagonists: Side-chain and backbone modifications
Satoshi Ueda, Shinya Oishi, Zi-xuan Wang, Hiroaki Ohno, Stephen C. Peiper, Nobutaka Fujii
Preparation of nucleoside analogs as potential precursors to modified polynucleotides
Kamal H. Bouhadir, Nadine Al-Khalil, Manal Farah, Fares A. Fares, Niveen Nasser
Synthesis and potency of Sansalvamide A derivatives in pancreatic cancers
Suchitra Ravula, Po-Shen Pan, Thomas J. Styers, Rodrigo Rodriguez, Emily Parry, Joseph D. Brown, Erin Singh, Chung-Mao Pan, Kathleen L. McGuire, Shelli R McAlpine
Intercalation of C60-carboxymethyl-b-cyclodextrin into magnesium-aluminum layered double hydroxide
Annette Medina, Melissa Martínez, Julissa R Gonzalez, Agustín Díaz, Jorge L. Colon
Limitations of the PAMPA assay and its role in drug discovery
Deborah Galinis-Luciani, Lorrie Nguyen, Mehran Yazdanian
Mesoporous silica nanoparticle-based system with double stranded oligonucleotides caps for reversible, controlled release of drugs and genes
Juan Luis Vivero-Escoto, Victor S-Y. Lin
Total synthesis and biological evaluation of Naamidine A and studies towards spiroleucettadine
Nicholas S. Aberle, Guillaume Lessene, Francesca Walker, Keith G. Watson
Pharmacophore design on the base of molecular recognition principles
Michael B. Darkhovskii, Felix S. Dukhovich
Multi-gram total syntheses of Zapotin and (±)-Abyssinone II, cancer chemopreventive natural products
Arup Maiti, John M. Pezzuto, Muriel Cuendet, Tamara Kondratyuk, Vicki L. Croy, Mark Cushman
Targeting protein kinase C (PKC) to specific cellular membrane domains with the use of DAG-lactones containing rigid oligo(p-phenylene ethynylene) acyl units
Dina M. Sigano, Krishnan Malolanarasimhan, Noemi Kedei, Nancy E. Lewin, Peter M. Blumberg, Victor E. Marquez
Design and development of new and efficient linkers for tumor-targeting drug delivery
Jin Chen, Xianrui Zhao, Shuyi Chen, Jennifer Curato, Robert Rutigliano, Dafna Bar-Sagi, Iwao Ojima
The design and synthesis of some novel bisphosphonates as potent inhibitors of farnesyl diphosphate synthase
Yonghui Zhang, Fenglin Yin, Rong Cao, Annette Leon-Rossell, Eric Oldfield
Parallel synthesis and high-throughput solubility determination of NCGC produced libraries: Models for probe development
Michael E. Nelson, Janak K. Padia, Karina M. Zuck, James Inglese, Christopher P. Austin
Activation of gene expression in living cells by a synthetic transcription factor mimic
Xiangshu Xiao, Peng Yu, Hyun-Suk Lim, Thomas Kodadek
Two approaches to synthesis of aryl sulfonyl chloride intermediate for Apratastat TMI-005
Joseph Zeldis, Lalitha Krishnan, T. Z. Wang, David Blum
Site-directed mutagenesis of the C1b domain of protein kinase C (PKC) delta provides a unique platform for the development of selective ligands for the atypical PKC zeta
Ji-Hye Kang, Megan L. Peach, Yongmei Pu, Peter M. Blumberg, Victor E. Marquez
Effects of cyclization constraints on helix/turn peptide structures
Renée L. Beyer, Huy N. Hoang, Giang T. Le, David P. Fairlie
Alpha helix induction in HIV REV34-50 by N-terminal nucleators
Renée L. Beyer, Michael J. Kelso, Robert C. Reid, Giang T. Le, David P. Fairlie
Reduction of aldehydes and ketones using solid supported borohydride and microwave heating
Panagiotis Ioannidis, Ronny Lundin, Pino Pilotti
New paradigm for high throughput preparative HPLC columns
Peter C Rahn, Tivadar Farcas, Gareth Friedlander, Joshua Heng, Emmet Welch
Compound enumeration in chemical patents
Mark R. Hansen, Richard JD Rouse, Hugo O. Villar
Sugar-coated nanobiotics
Sampath C. Abeylath
Intercalation of fulleropyrrolidines into zirconium phosphate layers for drug delivery applications
Melissa Martinez, Annette Medina, Agustín Díaz, Jorge L. Colon
Potent and selective 3-amino-1-cyclopentanecarboxamide CCR2 antagonists
Lihu Yang, Richard X. Jiao, Chris Moyes, Greg Morriello, Gabor Butora, K. Shankaran, Alexander Pasternak, Steve Goble, Changyou Zhou, Malcolm MacCoss, Anne-Marie Cumiskey, Larry Peterson, Mike Forrest, Pasquale P. Vicario, Julia M. Ayala, Hong Jin, Margaret A. Cascieri, Mary Struthers, Julie MeMartino, Sander G. Mills
Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 agonists leading to new spirocyclic antagonists
Alexander Pasternak, Steve Goble, Gabor Butora, George A. Doss, Nancy N. Tsou, Pasquale P. Vicario, Julia M. Ayala, Julie A. DeMartino, Sander G. Mills, Lihu Yang
3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor
Gabor Butora, Richard X. Jiao, William H. Parsons, Pasquale P. Vicario, Jin Hong, Julia M. Ayala, Margaret A. Cascieri, Lihu Yang
Discovery of Fms/Kit kinase inhibitors for the treatment of rheumatoid arthritis
Ryan Bremer, Jiazhong Zhang, Guoxian Wu, Yong Zhou, Angela Oh, Rafe Shellooe, Ivana Cheung, Kevin Eng, Betsy Burton, Catherine Luu, Marika Nespi, Hongyao Zhu, Maryam Tabrizizad, Julie De Joya-Rice, Kam Zhang, Clarence Hurt, Wayne Spevak, Rebecca Zuckerman, Weiru Wang, Chao Zhang, Ben Powell, Gaston Habets, Brian West, Gideon Bollag, D. Rick Artis, Prabha Ibrahim
Design, synthesis and study of new lipoxin A4 analogs
Nicos A. Petasis, Kalyan C. Nagulapalli, Raquel Keledjian, Rong Yang, Yee-Ping Sun, Charles N. Serhan
Synthesis and biological evaluation of phenylazo benzenesulfonamides as selective COX-2 inhibitors
Shwu-Jiuan Lin, Li-Ming Yang
5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors: Synthesis, SAR and molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile
Subas M. Sakya, Xinjun Hou, Martha L. Minich, Bryson Rast, Andrei Shavnya, Kristin M. L. DeMello, Hengmiao Cheng, Jin Li, Burton H. Jaynes, Donald W. Mann, Carol F. Petras, Scott B. Seibel, Suzanne St. Denis, Michelle L. Haven, Michael P. Lynch
1H-Pyrrole-2,5-dione derivatives as novel COX-2 inhibitors
Ji Y. Jeon, Kyung-J. Yun, Kyung-T. Lee, Jae Yeol Lee
Structural requirements for time-dependent and time-independent inhibition of prostaglandin synthase I (COX I)
Gianmarc G. Johns, Amanda E. Conway, Barry S. Selinsky
Discovery of novel, potent, and orally bioavailable STAT6 inhibitors
Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi, Shin-ichi Tsukamoto, Mitsuaki Ohta
Quinol-4-ones as dissociated non-steroidal glucocorticoid A-ring mimetics
Renee M. Zindell, John Regan, Thomas Lee, Younes Bekkali, Joerg Bentzien, Abdelhakim Hammach, Tom Kirrane, Daniel Kuzmich, John Proudfoot, Mark Ralph, Alison Capolino, Richard Nelson, Donald Souza, Dianne Thome, Gerald H. Nabozny, David Thomson
A high throughput, automated chemistry approach to the lead optimization of novel P38 MAP kinase inhibitors derived from 1,4-disubstituted naphthalenes
Hui Wu, Mark A. Ashwell, Yanbin Liu, Syed M. Ali, Jason Hill, Woj Wrona
Applying fragment based drug discovery: p38, a case study
Frank P. Hollinger, Zenon Konteatis, Jennifer L. Ludington, Michael Karpusas, Kristofer K. Moffett, Dan Nguyen, Michael S. Saporito, Katrina Northrop, Xiaomei Chai, Marina Bukhtiyarova, Matthew Clark, Frank Guarnieri, Enrique L. Michelotti, Eric Springman
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD
Laurent Provins, Michel Guyaux, Joel Mercier, Bernard Christophe, Michel Gillard, Sophie Jadot, Patrick Lo Brutto, Luc Quéré, Jean-Philippe Starck, Patrice Talaga
Synthesis of 1,3,4-thiadiazole and 1,3,4-oxadiazole containing butanoic acids as potent and selective αvβ3 integrin receptor antagonists
John A. Wendt, Heather G. Stenmark, Mark L. Boys, Lori Schretzman, Thomas D. Penning, Mark A. Russell, V. Wayne Engleman, Sandra K. Freeman, Melanie L. Hanneke, Marissa Westlin, Tiffany Duffin, Mary Beth Finn, Jeffery L. Keene, Kristen E. Shannon, Christina N. Steininger, Maureen A. Nickols, Jon A. Klover, William Westlin, G. Allen Nickols
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists
Vincent J Colandrea, Irene E Legiec, Pei Huo, Lin Yan, Jeffrey J. Hale, Sander G. Mills, James Bergstrom, Deborah Card, Gary Chrebet, Richard Hajdu, Carol Ann Keohane, James Milligan, Mark Rosenbach, Gan-Ju Shei, Suzanne Mandala
Selective S1P1 receptor antagonist: Synthesis and its in vivo effects
Sheng-Kai Wang, M. Germana Sanna, Yu-Hsien Chen, Pedro J. Gonzalez-Cabrera, Anthony Don, David Marsolais, Hugh Rosen, Chi-Huey Wong
Discovery, design and SAR studies of 1,2,4-oxadiazole based highly potent S1P1 receptor agonists with exceptional selectivity against S1P2 and S1P3
Zhen Li
Synthesis of the immunoproteasome catalytic subunit LMP2-specific modulators
Abby Ho, Kyung-Bo Kim
Caffeic acid phenethyl ester blocks allergic reaction in mouse model
Sae-Gwang Park, Da-Young Lee, In-Hak Choi, Su-Kil Seo, Soo-Woong Lee, Won-Kyo Jung, Se-Kwon Kim, Il-Whan Choi
Discovery of novel, orally available piperidine-containing CCR1 antagonists
Shou-Fu Lu, Yuo-Ling Chou, Wheeseong Lee, Xiaolin Liang, Gary B. Phillips, Sabine Schlyer, Robert G. Wei, Jinlou Xu, Hongyi Yu, Xue Snow Ge, Paymann Harirchian, Sofia Ribeiro, Babu Subramanyam, Janette Walters, Richard Horuk, Monica J. Kochanny
Paper Withdrawn
Studies on Bruton's tyrosine kinase, a target for rheumatoid arthritis
Zhengying Pan, Heleen Scheerens, Jonathan Li, Brian E Schultz, Paul A Sprengeler, Michael D Sweeney, Paul Grothaus, Douglas A Jeffery, Peter R Young, James T Palmer, Stacie A. Dalrymple
TACE inhibitors for RA
Chunchun Zhang, Jeremy I. Levin, Frank E. Lovering, Mark Behnke, Kaapjoo Park, LinHong Sun, Yi Zhu, Yuhua Zhang
Paper Withdrawn
Inhibitors of Tpl2 kinase: An approach towards treatment of RA
Junjun Wu, Rajeev Hotchandani, Adrian Huang, Yonghan Hu, Satenig Guler, Huan-Qui Li, Lin-Ling Lin, Steve Tam, Neal Green
1,3,5-Triazine derivatives as protein A mimetics for the treatment of autoimmune diseases
Boulos Zacharie, Nicole Wilb, Shaun D. Abbott, Jean-François Bienvenu, Alan Cameron, Josée Cloutier, Jean-Simon Duceppe, Abdallah Ezzitouni, Daniel Fortin, Jean-Hugues Fournier, Karine Houde, Caroline Lauzon, Joël Lechasseur, Nancie Moreau, Valérie Perron, Michel Asselin, Marie-Ève Fafard, Dannyck Gaudreau, Lilianne Geerts, Brigitte Grouix, François Sarra-Bournet, Natalie St-Amant, Lyne Gagnon, Christopher Penney
Arylaminoethyl succinamides as a novel series of noncovalent Cathepsin S inhibitors
Arnab K. Chatterjee, Hong Liu, David C Tully, Jianhua Guo, Robert Epple, Ross Russo, Jennifer A Williams, Glen Spraggon, Badry D. Bursulaya, Thomas Hollenbeck, Perry Gordon, Tove Tuntland, Jonathan Chang, Jun Li, Jennifer L. Harris
Potent and selective semicarbazide-sensitive amine oxidase (SSAO) inhibitors with anti-inflammatory activity
Eric Y Wang, Hongfeng Gao, Mary MacDonald, David S Jones, Huong-Thu Ton-Nu, Anne O'Rourke, Luisa Salter-Cid, Li Huang, Andrew Miller, Matthew D Linnik
Design and synthesis of small molecule TLR7 and TLR8 immune response modifiers: Investigation of novel A-ring substituted imidazo[4,5-c]quinolines
Michael J. Rice, Bryon A. Merrill, David S. Hays, Shri Niwas, Michael E. Danielson, Joshua R. Wurst, Gregory D. Lundquist, Chad A. Haraldson, John F. Gerster, Philip D. Heppner, Tushar A. Kshirsagar, Sarah C. Johannessen, Maureen A. Kavanagh, Kyle J. Lindstrom, Ryan B. Prince, David T. Amos, Matthew R. Radmer, David J. Squire, Scott E. Langer, John R. Jacobsen, Jason D. Bonk, Jason C. Anderson, Sarah A. Strong, Steven A. Van Keuren, Lindsay R. Wurst, Sheila J. Gibson
Novel heterocyclic TLR7 and TLR8 immune response modifiers: Design and synthesis of cytokine-inducing 2H-pyrazolo[3,4-c]quinolin-4-amines
David S. Hays, Michael E. Danielson, Chad A. Haraldson, Shri Niwas, John F. Gerster, Jason D. Bonk, Sonja J. Mackey, Kyle J. Lindstrom, Ryan B. Prince, Joan T. Moseman, Gregory D. Lundquist, Maureen A. Kavanagh, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Michael J. Rice, Joshua R. Wurst, Sarah J. Spessard, Matthew R. Radmer, Sarah A. Strong, David T. Amos, Daniel J. Willie, Lindsay R. Wurst, Sheila J. Gibson
Synthesis and SAR of TLR7 and TLR8 small molecule immune response modifiers: Novel alkylamino and alkoxy functionalized imidazo[4,5-c]quinolines
Larry R. Krepski, Karl J. Manske, George W. Griesgraber, Daniel E. Duffy, Joan T. Moseman, Luke T. Dressel, Doris Stoermer, Philip D. Heppner, Tushar A. Kshirsagar, Joseph F. Dellaria, Sheila J. Gibson, Lindsay R. Wurst
Design and synthesis of small molecule TLR7 and TLR8 immune response modifiers (IRMs): The preparation and biological evaluation of oxazino[4',3':1,2]imidazo[4,5-c]quinolines
George W. Griesgraber, Michael J. Rice, Sarah C. Johannessen, Tushar A. Kshirsagar, Michael E. Danielson, Peter V. Maye, John F. Gerster, Kyle J. Lindstrom, Azim C. Celebi, Michael J. Reiter, Lindsay R. Wurst, Sheila J. Gibson
Structure-activity relationships of inhibitors of microsomal prostaglandin E2 synthase derived from MK-886
Hélène Juteau, Yves Gareau, Sébastien Laliberté, Erich L. Grimm, Marc Blouin, Renee Aspiotis, D. Bruce Mackay, Rick W. Friesen, Diane Ethier, Joseph A. Mancini, Nathalie Methot, Joel Rubin, Jocelyne Guay, Sebastien Guiral, Denis Riendeau
Structure-activity relationships of inhibitors of microsomal prostaglandin E2 synthase identified from high-throughput screening
Tom Y-H. Wu, Hélène Juteau, Sebastien Guiral, Lynn Dufresne, Hugo Poirier, Yves Ducharme, Richard W. Friesen
Anti-sepsis compounds: Design, synthesis, and endotoxin-sequestering activities of novel lipopolyamine analogs
Sunil A. David, Anurupa Shrestha, Diptesh Sil, Ashok Adisechan, Apurba Datta, Thuan B. Nguyen, Matthew R. Kimbrell, Rajalakshmi Balakrishna
Design and synthesis of antiviral Ceragenins
Xinzhong Lai, Dianliang Geng, Derya Unumatz, Scott VanCompernolle, Paul B. Savage
Pyrroloquinolines as human cytomegalovirus polymerase inhibitors: SAR of arylethanolamine side-chain at C-8
Sajiv K. Nair, Brenda L. Schultz, James A. Nieman, Steven E. Heasley, Valerie A. Vaillancourt, Carolyn A. Brammer
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals
James A. Nieman, Steven E. Heasley, Sajiv K. Nair, Brenda L. Schultz, Herbert M. Zerth
Isoindolylureas a new group of antiviral compounds
Manjusha Verma, Krishna Nand Singh
Synthesis, anti-HIV and CD4 Down-modulation activities of novel CADA compounds
Thomas W. Bell, Sreenivasa Anugu, Noah Duffy, Kurt Vermeire, Dominique Schols
Synthesis and structure activity relationship of the first inverse agonists for the constitutively active viral-encoded receptor US28
Janneke W. Hulshof, Henry F. Vischer, Mark H. P. Verheij, Martine J. Smit, Iwan J. P. de Esch, Rob Leurs
Tight-binding fluorinated inhibitors of viral neuraminidase
Ahamindra Jain, Alexander D. Huters, Adam Weinstein, Daniel K. Kwan, Nisha Sandesara
Identification of a novel series of NNRTIs with broad antiviral potency against mutant genotypes associated with treatment failure
Serge R. Landry, Ma'an H. Amad, Pierre R. Bonneau, Josée Bordeleau, René Coulombe, Patrick L. DeRoy, Louise Doyon, Jianmin Duan, Anne-Marie Faucher, Alexandre Gagnon, Chantal Grand-Maître, Ingrid Guse, Araz Jakalian, Éric Jolicoeur, Steven R. Laplante, Éric Malenfant, Sébastien Morin, Julie Naud, Jeff A. O'Meara, Bruno Simoneau, Bounkham Thavonekham, Kimberley Thompson, Christiane Yoakim, Michael Boes, Michael G. Cordingley
Synthesis of 2-bromo-6-octylamino-1-β-D-ribofuranosylimidazo[4,5-e][1,3]diazepine-4,8-dione: A Ring-expanded nucleoside analog with a therapeutic promise against Flaviviridae
Peng Zhang, Ning Zhang, Ramachandra S. Hosmane
Synthesis and biological evaluation of a novel series of benzothiadiazines as hepatitis C virus RNA-dependent RNA polymerase inhibitors
Peggy P. Huang, John T. Randolph, Larry L. Klein, Debra A. Montgomery, Sherie V. Masse, Warren M. Kati, Hongmei Mo, Kent D. Stewart, David WA Beno, Dale J. Kempf
In vitro and in vivo activity of 2'-O-alkyl-4'-thio modified antisense oligonucleotides
Thazha P. Prakash, Prasad Dande, Andrew M. Siwkowski, Sam Lee, Hans J. Gaus, Eric E. Swayze, Balkrishen Bhat
Synthesis of 2'-deoxy-2'-fluoro-2'-C-methylcytidine from uridine as a potent hepatitis C virus inhibitor
Peiyuan Wang, Wojciech J. Stec, Michael J. Otto, Kyoichi A. Watanabe
L-3,6-dioxa-[3.2.0]bicyclonucleosides: Synthesis and biological evaluation
Xingang Fang, Raymond F. Schinazi, Dennis C. Liotta
Synthesis and anti-HCV activity of 4'-substituted nucleosides
Mark Smith, Joesph Martin, Dave Smith, Hans Maag, Isabel Naiera, Wen-Rong Jiang, Klaus Klumpp, Vincent Leveque, Nick Cammack, Nils Gunnar Johansson, Genadiy Kalayanov, Anna-Karin Belfrage, Kurt Benkestock, Kevin Farnell, Steven Hiscock, Björn Lindborg, Tatiana Maltseva, Veronique Morisson, Pedro Pinho, Christian Sund, Matt Tozer, Anna Winquist, Xiao-Xiong Zhou
Gem-dialkyl dihydronaphthylene-1, 3-dione benzothiadiazine derivatives as potent inhibitors of hepatitis C NS5B polymerase
Douglas K. Hutchinson, David W. A. Beno, Todd D. Bosse, Wenping He, Wen W. Jiang, Warren M. Kati, Larry L. Klein, William Kohlbrenner, Daniel P. Larson, Yaya Liu, Sherie V. Masse, Tim Middleton, Akhteruzzaman Molla, Debra A. Montgomery, Teresa Rosenberg, Kent D. Stewart, Vincent S. Stoll, Dale J. Kempf
Tertiary amine derivatives of 4,4-dialkyl-4H-naphthalene-1,3-dione-substituted benzothiadiazine inhibitors of hepatitis C NS5B polymerase
John T Randolph, Charles A Flentge, Peggy P Huang, Larry L Klein, Debra A Montgomery, Sherie V Masse, Warren M Kati, Hongmei Mo, Kent D Stewart, David W A Beno, Dale J Kempf
Inhibitors of HCV NS5B polymerase: Synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthylene benzothiadiazine derivatives
A. Chris Krueger, Darold L. Madigan, Todd D. Bosse, Wen W. Jiang, Warren M. Kati, Daniel P. Larson, Yaya Liu, Clarence J. Maring, Sherie Masse, Tim Middleton, Hongmei Mo, Akhteruzzaman Molla, Debra Montgomery, Dale J. Kempf
Discovery of VP19744: A pyrano[3,4-b]indole-based inhibitor of HCV NS5B polymerase demonstrating in vivo antiviral activity
Matthew G. LaPorte, Randy W. Jackson, Christopher J. Burns, Tandy L. Draper, Janet A. Gaboury, Kristin Galie, Torsten Herbertz, Alison R. Hussey, Susan R. Rippin, Christopher A. Benetatos, Srinivas K. Chunduru, Dorothy C. Young, Joel S. Christiansen, Glen A. Coburn, Christopher J. Rizzo, Marc S. Collett, Daniel C. Pevear, Stephen M. Condon
Synthesis and structure-activity relationship studies of benzimidazole and related compounds as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors
Takahiro Oka, Shintaro Hirashima, Kazutaka Ikegashira, Satoru Noji, Hiroshi Yamanaka, Yoshinori Hara, Tomio Ishida, Takayoshi Suzuki, Shinji Yata, Izuru Ando, Satoru Ikeda, Hiromasa Hashimoto
Discovery and design of potent piperidine-based CCR5 antagonists for the potential treatment of HIV-1 infection
Brian A. Chauder, Donald Anderson, Christopher J. Aquino, Neil Bifulco, Lawrence R. Boone, Eric E. Boros, Pek Y. Chong, Kien S. Du, Maosheng Duan, Robert G. Ferris, Wieslaw M. Kazmierski, Terrence P. Kenakin, Cecilia S. Koble, Daniel G. Lang, Jennifer P. Peckham, Andrew Spaltenstein, James B. Thompson, Michael K. Youngman, Patricia J. Wheelan
Hydrazone amides as novel peptoid surrogates for expedited library synthesis: Application to the preparation of TSG101-directed HIV-1 budding antagonists
Fa Liu, Andrew G. Stephen, Catherine Adamson, Eric O. Freed, Robert J. Fisher, Terrence R. Burke Jr.
Design, synthesis and antiviral activity of cyclobutyl phosphonate nucleoside analogs as chain terminators against HIV
Yongfeng Li, Raymond F. Schinazi, Dennis C. Liotta
Design and discovery of second generation HIV-1 integrase inhibitors as anti-HIV/AIDS agents
Raveendra Dayam, Tino Sanchez, Laith Q Al-Mawsawi, Nouri Neamati
Virtual screening application of a model of full-length HIV-1 integrase complexed with viral DNA
Iwona E Weidlich, Rajeshri G. Karki, Marc C. Nicklaus
Bicyclic pyrimidones as inhibitors of HIV-integrase
Benedetta Crescenzi, Cristina Gardelli, Monica Donghi, Marco Ferrara, Paola Pace, Olaf Kinzel, Ester Muraglia, Michael Rowley, Ralph Laufer, Fabrizio Fiore, Odalys Gonzalez Paz, Massimiliano Fonsi, Kara A. Stillmock, Marc V. Witmer, Daria J. Hazuda, Vincenzo Summa
Click chemistry-derived biotin-tagged diketo acid-containing biphenyl ketones designed as HIV-1 integrase photoaffinity ligands
Xue Zhi Zhao, Elena A. Semenova, Allison Johnson, Christophe Marchand, Chenzhong Liao, Marc C Nicklaus, Yves Pommier, Terrence R Burke Jr.
Novel HIV-1 integrase inhibitors: 8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-ones
Boyoung Kim, Thorsten E. Fisher, Terry A. Lyle, Steven D. Young, Joseph P. Vacca, Daria J. Hazuda, Peter J. Felock, William A. Schleif, Lori Gabryelski, John S. Wai
Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors
H. Marie Moritz, Peter Williams, John S. Wai, Janetta M. Dewhurst, Terry A. Lyle, Carl F. Homnick, Joseph P. Vacca, Daria J. Hazuda, Peter J. Felock, Kara A. Stillmock, William A. Schleif, Lori J. Gabryelski
Synthesis and biological activity of L-chicoric acid analogs as HIV-1 integrase inhibitors
Xiangyang Lei, Charles G. Gibbs, Manfred G. Reinecke, W. Edward Robinson Jr.
Synthesis and activity of thiadiazines as HCV polymerase inhibitors
Keith F. McDaniel, Allan C. Krueger, David A. Betebenner, Pamela L. Donner, Brian E. Green, Darold L. Madigan, Clarence J. Maring, Debra A. Montgomery, Tim R. Middleton, Warren M. Kati, Gennadiy Koev, Wen W. Jiang, Yaya Liu, Hongmei Mo
Development of QPLD (QM-polarized ligand docking)
Art E. Cho, Ramy Farid, Richard Friesner
Norcysteine (α-thiolglycine), a versatile scaffold to tailor structure and activity of peptides
Manoj P. Samant, Doley J. Hong, Glenn Croston, Jean E. Rivier
Development of a new cancer screening method by comprehensive 2D gas chromatography/time-of-flight mass spectrometry (GCxGC/TOF MS)
J. M. D. Dimandja, I Enwerem
Protein-binding agents based on the supramolecular self-assembly of oligonucleotide-linked organic fragments
Andrew Hamilton, Debarati M. Tagore, Katherine I Sprinz, Steven Fletcher
Chemical validation of novel hydrogenation, ozonolysis, and high pressure microfluidic reactors as new tools for medicinal synthetic chemistry
Richard Jones, Ferenc Darvas, Csaba Csajagi
Pattern analysis using NMR spectroscopy (PANSY): Applications to organic and pharmaceutical chemistry
Ruben M. Savizky, John L. Bove, Zhen Y. Liu
Synthesis of selectively protected spirostane-2,3-diol stereoisomers
Katharine L. Bowdy, Branko S. Jursic
The metal-complexation properties of cytotoxic tripodal hexadentate chelators: Effects of heterocycle donor arms on Fe(II) chelation and fibroblast IC50 value
Roy P. Planalp, Giang Lu, Daniel P Kennedy, Martin W. Brechbiel, Robin D. Rogers, Rong Ma, Frank M. Torti, Suzy V. Torti
Photogenerated bases for parallel microarray synthesis using Fmoc-chemistry
Wu Yao, Xiaolian Gao, Ailing Hong, Xiaochuan Zhou, Erdogan Gulari

Symposium Grid -- Division of Medicinal Chemistry -- Session Listing

Symposium Grid -- Drug Discovery -- Session Listing

The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006