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

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.

SUBMITTER: Sun W 

PROVIDER: S-EPMC2795317 | biostudies-literature | 2009 Feb

REPOSITORIES: biostudies-literature

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

Sun Wei W   Nikolovska-Coleska Zaneta Z   Qin Dongguang D   Sun Haiying H   Yang Chao-Yie CY   Bai Longchuang L   Qiu Su S   Wang You Y   Ma Dawei D   Wang Shaomeng S  

Journal of medicinal chemistry 20090201 3

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. ...[more]

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