Synthesis and cytotoxicity studies of novel sansalvamide A derivatives

MEDI 325

Yalda S. Mostofi, aztec_yalda@hotmail.com1, Suchitra Ravula2, Stephanie Lapera, stephanielapera@hotmail.com2, Melinda R. Davis, melindarenee@gmail.com2, William S. Disman2, Katerina Otrubova, kotrubova@hotmail.com2, Erinprit Signh2, and Shelli R McAlpine2. (1) Department of chemistry and biochemistry, SDSU, 5500 Campanile Drive, San Diego, CA 92182-1030, (2) Department of Chemistry and Biochemistry, San Diego State University, 5500 Campanile Drive, San Diego, CA 92182-1030
Colon cancer is the third most common form of cancer and the second leading cause of death among cancers. Pancreatic cancer is the fifth most deadly cancer each year 32,000 individuals in the U.S. are diagnosed with this condition. It has been shown that Sansalvamide A (San A), which is a depsipeptide isolated from marine fungus, exhibits anti-tumor activity. In recent years, we have synthesized a series of San A derivatives that have been optimized for potency against drug-resistant pancreatic and colon cancers. Results from our laboratory indicate that molecules belonging to our San A library produce effective inhibitors in the nanomolar concentration ranges against these cancers. These molecules represent a significant breakthrough because the clinically used agent for these drug-resistant cancers manifest significantly greater IC50 values against these same cell lines proving San A to be a promising class of anti-tumor agents.
 

Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007