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Published on: November 30, 2022
Synthesis and evaluation of Apogossypol atropisomers as potential Bcl-xL antagonists
Jun Wei1, Michele F Rega, Shinichi Kitada
1Burnham Institute for Medical Research, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA.
Abstract:
Anti-apoptotic Bcl-2 family proteins such as Bcl-2 and Bcl-X(L) have been recently validated as targets for the discovery of novel anti-cancer agents. We previously reported that racemic (+/-) Apogossypol, a semi-synthetic compound derived from the natural product Gossypol, binds and inhibits Bcl-2 and Bcl-X(L)in vitro and in cell. Given that (+) and (-) Gossypol display different proapoptotic activities, here we report on the synthesis of (+) and (-) Apogossypol and the evaluation of their in vitro and cellular activity.
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