Document Report Card

ID: ALA1143377

Journal: J Med Chem

Title: Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.

Authors: Sun W, Nikolovska-Coleska Z, Qin D, Sun H, Yang CY, Bai L, Qiu S, Wang Y, Ma D, Wang S.

Abstract: A series of new Smac mimetics have been designed, synthesized, and evaluated. The most potent compound 10 binds to XIAP, cIAP-1, and cIAP-2 BIR3 proteins with K(i) of 3.9, 0.37, and 0.25 nM, respectively. Compound 10 antagonizes XIAP in a cell-free functional assay and induces rapid cIAP-1 degradation in cancer cells. Compound 10 inhibits cell growth in the MDA-MB-231 cancer cell line with an IC(50) of 8.9 nM.

CiteXplore: 19138149

DOI: 10.1021/jm801101z