1239670-64-4Relevant articles and documents
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins
Sun, Haiying,Lu, Jianfeng,Liu, Liu,Yi, Han,Qiu, Su,Yang, Chao-Yie,Deschamps, Jeffrey R.,Wang, Shaomeng
, p. 6361 - 6367 (2010)
A series of compounds were designed and synthesized as antagonists of cIAP-1/2 and XIAP based upon our previously identified lead compound SM-122 (1). The most potent of these (7) binds to XIAP, cIAP-1, and cIAP-2 proteins with Ki values of 36, a cell-free caspase-9 functional assay, efficiently induces cIAP-1 degradation in cells at concentrations as low as 10 nM, and triggers activation of caspases and PARP cleavage in the MDA-MB-231 breast cancer cell line. Compound 7 potently inhibits cell growth in the MDA-MB-231 cancer cell line with an IC50 value of 200 nM and is 9 times more potent than compound 1.