2. Academic Validation
  3. Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction

Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction

  • J Med Chem. 2009 Dec 24;52(24):7970-3. doi: 10.1021/jm901400z.
Shanghai Yu 1,  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
Affiliations

Affiliation

  • 1 Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, USA.
PMID: 19928922 DOI: 10.1021/jm901400z
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.

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