| Literature DB >> 19928922 |
Shanghai Yu1, Dongguang Qin, Sanjeev Shangary, Jianyong Chen, Guoping Wang, Ke Ding, Donna McEachern, Su Qiu, Zaneta Nikolovska-Coleska, Rebecca Miller, Sanmao Kang, Dajun Yang, Shaomeng Wang.
Abstract
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) 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 over tumor cells with mutated/deleted p53. Compound 5 has a good oral bioavailability and effectively inhibits tumor growth in the SJSA-1 xenograft model.Entities:
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Year: 2009 PMID： 19928922 PMCID： PMC2795799 DOI： 10.1021/jm901400z
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446