Pyrogallol-Based Molecules as Potent Inhibitors of the Antiapoptotic Bcl-2 Proteins
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- 作者：Guozhi Tang ; Chao-Yie Yang ; Zaneta Nikolovska-Coleska ; Jie Guo ; Su Qiu ; Renxiao Wang ; Wei Gao ; Guoping Wang ; Jeanne Stuckey ; Krzysztof Krajewski ; Sheng Jiang ; Peter P. Roller ; Shaomeng Wang
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：April 19, 2007
- 年：2007
- 卷：50
- 期：8
- 页码：1723 - 1726
- 全文大小：303K
- 年卷期：v.50,no.8(April 19, 2007)
- ISSN：1520-4804
文摘
We report herein a new class of small-molecule inhibitorsof antiapoptotic Bcl-2 proteins. The most potent compound, 7, bindsto Bcl-2, Bcl-xL, and Mcl-1 proteins with Ki of 110, 638, and 150 nM,respectively. Compound 7 is highly effective in induction of cell deathin breast cancer cells with high levels of Bcl-2, Bcl-xL, and Mcl-1proteins and represents a promising lead compound for the design ofnew anticancer drugs.