Synthesis and evaluation of Apogossypol atropisomers as potential Bcl-xL antagonists.

Jun Wei, Michele F Rega, Shinichi Kitada, Hongbin Yuan, Dayong Zhai, Prabhakar Risbood, Herbert H Seltzman, Charles E Twine, John C Reed, Maurizio Pellecchia

Cancer letters 2009 Jan 08

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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.

Citation

Jun Wei, Michele F Rega, Shinichi Kitada, Hongbin Yuan, Dayong Zhai, Prabhakar Risbood, Herbert H Seltzman, Charles E Twine, John C Reed, Maurizio Pellecchia. Synthesis and evaluation of Apogossypol atropisomers as potential Bcl-xL antagonists. Cancer letters. 2009 Jan 08;273(1):107-13