Design, Synthesis, and Evaluation of Potent, Nonpeptidic Mimetics of Second Mitochondria-Derived Activator of Caspases.

[摘要]：A series of new Smac mimetics have been designed, synthesized, and evaluated. The most potent compd. 10 (I) binds to XIAP, cIAP-1, and cIAP-2 BIR3 proteins with Ki of 3.9, 0.37, and 0.25 nM, resp. Compd. 10 antagonizes XIAP in a cell-free functional assay and induces rapid cIAP-1 degrdn. in cancer cells. Compd. 10 inhibits cell growth in the MDA-MB-231 cancer cell line with an IC50 of 8.9 nM.

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