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

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

  • J Med Chem. 2009 Feb 12;52(3):593-6. doi: 10.1021/jm801101z.
Wei Sun 1,  Zaneta Nikolovska-Coleska,  Dongguang Qin,  Haiying Sun,  Chao-Yie Yang,  Longchuang Bai,  Su Qiu,  You Wang,  Dawei Ma,  Shaomeng Wang
Affiliations

Affiliation

  • 1 State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China.
PMID: 19138149 DOI: 10.1021/jm801101z
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.

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