913961-18-9Relevant articles and documents
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins
Wang, Guoping,Nikolovska-Coleska, Zaneta,Yang, Chao-Yie,Wang, Renxiao,Tang, Guozhi,Guo, Jie,Shangary, Sanjeev,Qiu, Su,Gao, Wei,Yang, Dajun,Meagher, Jennifer,Stuckey, Jeanne,Krajewski, Krzysztof,Jiang, Sheng,Roller, Peter P.,Abaan, Hatice Ozel,Tomita, York,Wang, Shaomeng
, p. 6139 - 6142 (2006)
A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2. The most potent compound 5 (TW-37) binds to Bcl-2 with a Ki value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner.