| MEDI | Monday, 11 September 2006 | ||
8:00 PM-10:00 PM Moscone Center -- Hall D, Sci-Mix | |||
Sci-Mix | |||
| Organizer: | David P. Rotella | ||
| 261 | Photogenerated bases for parallel microarray synthesis using Fmoc-chemistry Wu Yao, Xiaolian Gao, Ailing Hong, Xiaochuan Zhou, Erdogan Gulari | ||
| 442 | 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing A 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators Puwen Zhang, Jeffrey C. Kern, Eugene A. Terefenko, Andrew Fensome, Ray J Unwalla, Yuan Zhu, Jeff Cohen, Richard C. Winneker, Zhiming Zhang, Jay Wrobel | ||
| 416 | 3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogs as DPP-IV inhibitors for the treatment of type-II diabetes Hsing-Pang Hsieh, Mohane S. Coumar, Chung-Nien chang, Ssu-Hui Wu, Xin Chen, Chiung-Tong Chen, Weir-Torn Jiaang | ||
| 326 | De Novo design and synthesis of novel RNA polymerase inhibitors as potential anti-tuberculosis agents Anil K. Agarwal, Julian G. Hurdle, Amer I. AlOmar, Ian Chopra, A Peter Johnson, Colin W. G. Fishwick | ||
| 198 | 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 | ||
| 539 | A quantum dot DNA aptamer linked system for detecting proteins Eric Holwitt, Veronica Franz | ||
| 558 | A success story of fragment-based lead generation at Astrazeneca Loredana Spadola, Morten Hohwy, Karl Edman | ||
| 337 | Antibacterial agents from multivalent design of antimicrobial peptides and combinatorial library screening Zhigang Liu, Chunhui Zhou, Anne Young, Heather Deshazer, Amanda Rice, Neville R Kallenbach | ||
| 214 | 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 | ||
| 450 | Biaryl thiazolidin-2,4-diones: A new class of voltage-gated sodium channel blockers for treatment of neuropathic pain P. K. Chakravarty, C. H. Kuo, S. Tyagarajan, M. Ayer, W. H. Parsons, M. H. Fisher, M. J. Wyvratt, K. A. Lyons, Birgit T. Priest, Richard M. Brochu, I. E. Dick, G. J. Kaczorowski, E. McGowan, Nina Jochnowitz, J. W. Tarpley, S. West, B. S. Reiseter, Catherine Abbadie, W. J. Martin | ||
| 206 | 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 | ||
| 561 | Cellular delivery of phosphopeptides by positively-charged tripodal peptides Guofeng Ye, Nguyen H. Nam, Anil Kumar, Keykavous Parang | ||
| 508 | Design and development of cyclic amine BACE1 inhibitors: An overview Jared Cumming, Lingyan Wang, Suresh Babu, Carolyn Carroll, Xia Chen, Paul Gaspari, William Greenlee, Tao Guo, Doug Hobbs, Ying Huang, Ulrich Iserloh, Matthew Kennedy, Reshma Kuvelkar, Thuy Le, Guoqing Li, Jeffrey Lowrie, Lynne Ozgur, Jianping Pan, Kurt Saionz, Corey Strickland, Andrew Stamford, Dawit Tadesse, Johannes Voigt, Yusheng Wu | ||
| 484 | Design and synthesis of novel inhibitors of fatty acid amide hydrolase Joie Garfunkle, F. Anthony Romero, Dale L. Boger | ||
| 407 | Design and synthesis of potent and selective 5-HT2c receptor agonists Guohua Zhao, Chet Y. Kwon, Sharon N. Bisaha, Philip D. Stein, Chen-Pin Hung, Ginger Wu, Thao Ung, Xueying Cao, Keith J. Miller, Sarah Malmstrom, Ge Zhang, Eva Otanyi, William J. Keim, Mary Jane Cullen, Kenneth W. Rohrbach, Jinping Gan, Mary Ann Pelleymounter, Jeffrey A. Robl | ||
| 119 | Design and synthesis of target kinase inhibitor library Q. John Yu, Faming Zhang | ||
| 161 | 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 | ||
| 51 | Development of a novel carbohydrate microarray and its application in cancer diagnostics and therapeutics Joseph C. Manimala, Tim Roach, Zhitao Li, Jeffrey C. Gildersleeve | ||
| 370 | Development of new anti-malarial drugs derived from chloroquine Kekeli Ekoue-kovi, John, N Alumasa, Jayakumar K. Natarajan, Paul D. Roepe, Christian Wolf, Kimberly, S Yearick | ||
| 46 | 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 | ||
| 211 | Paper Withdrawn | ||
| 190 | 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 | ||
| 142 | Discovery of novel antitumor antimitotic agents that also reverse tumor resistance Aleem Gangjee, Jianming Yu, Staci N. Keller, Charles D. Smith | ||
| 92 | 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 | ||
| 365 | Drug discovery targeted the GHKL superfamily Xinshan Kang, Boris Klebansky, Richard Fine | ||
| 32 | Dual-targeting taxoid anticancer drug conjugates Stanislav Jaracz, Iwao Ojima | ||
| 75 | 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 | ||
| 543 | Fluorescence polarization (FP) assay for identification of vitamin D receptor (VDR) ligands Steven R. Duff, James G. Farnham, Bryan D. Marks, Naveeda Qadir, Hildegard C. Eliason, Mohammed Saleh Shekhani, Christina Fernandez-Perez, Kurt W. Vogel, William J. Frazee | ||
| 529 | Fluorescent probes to study serine/threonine phosphatases Fengtian Xue, Christopher T. Seto | ||
| 87 | 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 | ||
| 400 | Hit to lead discovery of potent 11b-HSD1 inhibitors Ravi Kurukulasuriya, Vince S. C. Yeh, William J. Chiou, Steven Fung, Jiahong Wang, Hing L. Sham, James T. Link | ||
| 136 | Hsp90 inhibitors: A study of coumarin antibiotic derivatives Donna J. Lubbers, Joseph A. Burlison, Brian S. J. Blagg | ||
| 537 | Medicinal chemistry refinement of a lead compound improves ex vivo metabolic stability with retention of in vivo functions and bioavailability Laura K. Wing, Hantamalala Ralay Ranaivo, Heather A. Behanna, Wenhui Hu, Sakti M. Roy, Danielle English, D. Martin Watterson | ||
| 172 | 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 | ||
| 62 | 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 | ||
| 80 | Novel non-steroidal/non-anilide type androgen antagonists effective toward mutated androgen receptor Aya Tanatani, Ken-ichi Wakabayashi, Hiroyuki Miyachi, Yuichi Hashimoto | ||
| 478 | Novel piperidine scaffold as an orally active NK1 antagonist Jonathan R. Young, Ronsar Eid, Robert J. DeVita, Gary G. Chicchi, Kwei-Lan C Tsao, Marc Kurtz, James V. Pivnichny, Sharon Tong, Song Zheng, Alan Wheeldon, Emma Carlson, Jerry Di Salvo, Ruth Kilburn, Alana Upthagrove, Sanjeev Kumar, Sander G. Mills | ||
| 137 | Novobiocin analogs: Development and evaluation of novel small molecule Hsp90 inhibitors Joseph A. Burlison, Donna J. Lubbers, Brian S. J. Blagg | ||
| 428 | P2Y1 antagonists: An analysis of the structural elements of ligand recognition based on molecular docking and 3D-QSAR Stefano Costanzi, Michihiro Ohno, Eun Joo Roh, Bhalchandra V. Joshi, Anny-Odile Colson, Dayle Houston, Savitri Maddileti, T. Kendall Harden, Kenneth Jacobson | ||
| 176 | 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 | ||
| 345 | Peptidyl vinyl sulfonyl inhibitors of cysteine protease: Development and biologically activity Michael H. Ober, Yen Ting Chen, Elizabeth Hansell, James H. McKerrow, William R. Roush | ||
| 329 | Phenylimidazole and 4-pyridone hybrid derivatives as novel inhibitors of bacterial enoyl-ACP reductases FabI and FabK Hideo Kitagawa, Tomohiro Ozawa, Sho Takahata, Maiko Iida, Jun Saito, Takashi Watanabe, Eiki Shitara | ||
| 540 | Polyketide engineering to supply advanced, complex scaffolds for the construction of high diversity, natural product-like combinatorial libraries Jasmina Nikodinovic, Bradley A. Bessette Jr., James E Cox, Stephen C. Bergmeier, Mark C. McMills, Nigel D Priestley, Dennis L Wright | ||
| 474 | Prodrugs of 3-(3,4-dicholorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane- 2,6-dicarboxylic acid (MGS0039): Potent and orally active group II mGluR antagonist with antidepressant-like potential Akito Yasuhara, Masato Nakamura, Kazunari Sakagami, Yasunori Kawakita, Toshiharu Shimazaki, Shigeyuki Chaki, Hiroshi Ohta, Atsuro Nakazato | ||
| 163 | Reactivity, selectivity and compatibility: A practical review of polymer supported coupling reagents Paul A Boguszewski, Alasdair A MacDonald, Aubrey J Mendonca, Frank P Warner | ||
| 394 | Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties James R. Corte, Tianan Fang, Donald J. P. Pinto, Wei Han, Zilun Hu, Xiang-Jun Jiang, Yun-Long Li, Alan R. Rendina, Joseph M. Luettgen, Pancras C. Wong, Kan He, Chong-Hwan Chang, Daniel L. Cheney, Robert M. Knabb, Ruth R. Wexler, Patrick Y. S. Lam, Jolicia F. Gauuan, Mark Hadden, Darren Orton | ||
| 48 | Successful delivery of siRNA to human chronic myelogenous leukemia cells by cobalamin-mediated endocytosis Randy Y. Adachi, Charles B. Grissom | ||
| 185 | Sugar-coated nanobiotics Sampath C. Abeylath | ||
| 490 | Synthesis and biological evaluation of a new series of nicotinic acetylcholine receptor (nAChR) ligands for positron emission tomography (PET) Yongjun Gao, Hayden T Ravert, Daniel Holt, John Hilton, Chris Endres, Mohab Alexander, Anil Kumar, Arman Rahmim, Hiroto Kuwabara, Dean F. Wong, Robert F. Dannals, Andrew G. Horti | ||
| 157 | Synthesis and evaluation of Estradiol-PEG-DNA alkylation agents using click chemistry Edward Y. Hua, David C. Labaree, Richard B. Hochberg, Robert N. Hanson | ||
| 525 | Synthesis and guanase inhibition studies of heterocycles and nucleosides containing the imidazo[4,5-d]pyridazine ring system Ravi K. Ujjinamatada, Ramachandra S. Hosmane | ||
| 386 | Synthesis and LXR activity of 3-[substituted phenyl] quinolines John W. Ullrich, Robert L. Morris, Ronald C. Bernotas, David Kaufman, Ponnal Nambi, Elaine Quinet, Liang Chen, Anita Halpern, Qiang-Yuan Liu, Dawn Savio, Mike Basso, Ray J Unwalla, Anna Wilhelmsson, Annika Goos Nilsson, Crina Ursu, Erik Arnelof, Johnny Sandberg, Christopher Enroth, Jay Wrobel | ||
| 228 | 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 | ||
| 26 | Synthesis of fluorinated tetraphenylporphyrins for potential use in photodynamic therapy Kip Conner, Valentina Tan, Meden Isaac, Ursula Simonis | ||
| 351 | Synthesis of phosphorous-containing folate and methotrexate analogs as potential inhibitors of dihydrofolate synthetase and antimalarial drugs Yonghong Yang, James K. Coward | ||
| 99 | Theoretical design of a novel series of enediynes containing metal center Edyta M. Brzostowska, Roald Hoffmann | ||
| 118 | 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 Pittalą, Mario Varasi, Juergen Moll, Fulvia Roletto, Patrizia Carpinelli, Paola Storici, Paolo Cappella, Daniele Fancelli | ||
| 229 | Tight-binding fluorinated inhibitors of viral neuraminidase Ahamindra Jain, Alexander D. Huters, Adam Weinstein, Daniel K. Kwan, Nisha Sandesara | ||
| 385 | Toward PPAR agonists as novel therapeutics for inflammation and CNS disorders Upasana Mehra, Jack J. Lin, Gaston Habets, Prabha N. Ibrahim, Rick Artis, Chao Zhang | ||
| 109 | 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 | ||
Symposium Grid -- Division of Medicinal Chemistry -- Session Listing
The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006