Synthesis of novel bio-active indolocarbazoles

ORGN 131

Sudipta Roy1, Alan Eastman2, and Gordon W. Gribble, GGribble@dartmouth.edu1. (1) Department of Chemistry, Dartmouth College, Hanover, NH 03755, (2) Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, NH 03755
Gö6976 was found to be a very potent checkpoint inhibitor even in presence of human serum and has been shown to potently inhibit Chk1. In our search for more potent and selective inhibitors, we will present the synthesis of 7-keto analogs of Gö6976. The synthesis involves the coupling of pre-formed indole units followed by the efficient oxidative cyclization using palladium triflate. The progress towards the synthesis of Gö6976 homologs will also be presented.

 

Heterocycles, Aromatics, Materials, Devices, Switches, Combinatorial Chemistry, Metal-Mediated Reactions
8:00 PM-10:00 PM, Sunday, 13 March 2005 Convention Center -- Hall D, Poster

Division of Organic Chemistry

The 229th ACS National Meeting, in San Diego, CA, March 13-17, 2005