Wei Jun, Rega Michele F, Kitada Shinichi, Yuan Hongbin, Zhai Dayong, Risbood Prabhakar, Seltzman Herbert H, Twine Charles E, Reed John C, Pellecchia Maurizio
Burnham Institute for Medical Research, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA.
Cancer Lett. 2009 Jan 8;273(1):107-13. doi: 10.1016/j.canlet.2008.07.031. Epub 2008 Sep 7.
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.
抗凋亡的Bcl-2家族蛋白,如Bcl-2和Bcl-X(L),最近已被确认为新型抗癌药物研发的靶点。我们之前报道过,外消旋(+/-) 去甲棉酚,一种从天然产物棉酚衍生而来的半合成化合物,在体外和细胞内均能结合并抑制Bcl-2和Bcl-X(L)。鉴于(+)和(-)棉酚表现出不同的促凋亡活性,在此我们报道(+)和(-)去甲棉酚的合成及其体外和细胞活性的评估。