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J Med Chem. 2006 Oct 19;49(21):6139-42.

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.

Author information

1
Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, USA.

Abstract

A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2. The most potent compound 5 (TW-37) binds to Bcl-2 with a K(i) value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner.

PMID:
17034116
DOI:
10.1021/jm060460o
[Indexed for MEDLINE]

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