Potent and Orally Active Small-Molecule Inhibitors of the MDM2-p53 Interaction

We report herein the design of potent and orally active small-molecule inhibitors of the MDM2-p53 interaction. Compound 5 binds to MDM2 with a K(i) value of 0.6 nM, activates p53 at concentrations as low as 40 nM, and potently and selectively inhibits cell growth in tumor cells with wild-type p53 ov...

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Detalhes bibliográficos
Main Authors: Yu, Shanghai, Qin, Dongguang, Shangary, Sanjeev, Chen, Jianyong, Wang, Guoping, Ding, Ke, McEachern, Donna, Qiu, Su, Nikolovska-Coleska, Zaneta, Miller, Rebecca, Kang, Sanmao, Yang, Dajun, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado em: 2009
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2795799/
https://ncbi.nlm.nih.gov/pubmed/19928922
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm901400z
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