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

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.

SUBMITTER: Wei J

PROVIDER: S-EPMC2653056 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature

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

Wei Jun J Rega Michele F MF Kitada Shinichi S Yuan Hongbin H Zhai Dayong D Risbood Prabhakar P Seltzman Herbert H HH Twine Charles E CE Reed John C JC Pellecchia Maurizio M

Cancer letters 20080907 1

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 v ...[more]

PMID: 18782651

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