Potent, Orally Bioavailable Diazabicyclic Small-Molecule Mimetics of Second Mitochondria-derived Activator of Caspases

A series of small-molecule Smac mimetics containing a diazabicyclic core structure have been designed, synthesized and evaluated. The most potent compound (6) binds to XIAP, cIAP-1 and cIAP-2 with K(i) values of 8.4, 1.5 and 4.2 nM, respectively, directly antagonizes XIAP in a cell-free functional a...

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Autori principali: Peng, Yuefeng, Sun, Haiying, Nikolovska-Coleska, Zaneta, Qiu, Su, Yang, Chao-Yie, Lu, Jianfeng, Cai, Qian, Yi, Han, Kang, Sanmao, Yang, Dajun, Wang, Shaomeng
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2008
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC2679375/
https://ncbi.nlm.nih.gov/pubmed/19049347
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm801254r
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