Synthesis of FR235222 derivatives: Novel templates as potent anticancer agents

ORGN 141

Stephanie Lapera, stephanielapera@hotmail.com, Chung-Mao Pan, Erin Singh, Suchitra Ravula, Po-Shen Pan, and Shelli R. McAlpine, mcalpine@chemistry.sdsu.edu. Department of Chemistry and Biochemistry, San Diego State University, 5500 Campanile Drive, San Diego, CA 92182-1030
The FR235222 structure represents a novel scaffold that targets human histone deacetylases (HDACs). HDACs regulate transcription of genes and represent a promising class of anticancer agents. HDACs are up-regulated in pancreatic cancers, and inhibiting these enzymes may lead to the control of cell growth. Thus, development of new structures that target HDACs may provide compounds that selectively target pancreatic cancer cells over normal cells. The synthesis of a series of FR235222 derivatives and the results of these compounds run in pancreatic cytotoxicity assays are described.