Design, Synthesis and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-derived Activator of Caspases

A series of tricyclic, conformationally constrained Smac mimetics have been designed, synthesized and evaluated. The most potent compound 6 (WS-5) binds to XIAP, cIAP-1 and cIAP-2 with K(i) values of 18, 1.1 and 4.2 nM, respectively. Compound 6 antagonizes XIAP in a functional assay and induces cIAP...

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Hauptverfasser: Zhang, Bin, Nikolovska-Coleska, Zaneta, Zhang, Yan, Bai, Longchuan, Qiu, Su, Yang, Chao-Yie, Sun, Haiying, Wang, Shaomeng, Wu, Yikang
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2008
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2662380/
https://ncbi.nlm.nih.gov/pubmed/19012392
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm801146d
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