Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 24, Pages 7970-7973Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901400z
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Funding
- National Cancer Institute, National Institutes of Health [R01CA121279, P50CA06956, P50CA097248]
- University of Michigan Cancer Center [P30CA046592]
- Prostate Cancer Foundation
- Leukemia and Lymphoma Society
- Ascenta Therapeutics, Inc
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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 its 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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