Author/Authors :
Wei، نويسنده , , Jun and Rega، نويسنده , , Michele F. and Kitada، نويسنده , , Shinichi and Yuan، نويسنده , , Hongbin and Zhai، نويسنده , , Dayong and Risbood، نويسنده , , Prabhakar and Seltzman، نويسنده , , Herbert H. and Twine، نويسنده , , Charles E. and Reed، نويسنده , , John C. and Pellecchia، نويسنده , , Maurizio، نويسنده ,
Abstract :
Anti-apoptotic Bcl-2 family proteins such as Bcl-2 and Bcl-XL 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-XL 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.
Keywords :
Apogossypol atropisomers , gossypol , Apogossypol , Mcl-1 , chemotherapy , Bcl-XL , apoptosis , bcl-2
