期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 4, 页码 717-720出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm701358v
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资金
- NCI NIH HHS [U19CA113317] Funding Source: Medline
A series of acylpyrogallols were designed, synthesized, and evaluated as small-molecule inhibitors of antiapoptotic Bcl-2 proteins. The most potent compound 9 (TM-179) binds to Bcl-2 with an IC50 of 170 nM and to Mcl-1 with a K-i of 37 nM. Compound 9 potently inhibits cell growth and induces apoptosis in human breast and prostate cancer cell lines.
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