Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins
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DOI：
10.1021/jm061400l
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发表时间：
2007-04-19
影响因子：
7.3
通讯作者：
Wang, Shaomeng
中科院分区：
文献类型：
--
作者：
Tang, Guozhi;Yang, Chao-Yie;Wang, Shaomeng
我们在此报道了一类新的抗凋亡Bcl-2蛋白的小分子抑制剂。最有效的化合物7与Bcl-2、Bcl-xL和Mcl-1蛋白结合，其K-i分别为110、638和150 nM。化合物7在具有高水平Bcl-2、Bcl-xL和Mcl-1蛋白的乳腺癌细胞中诱导细胞死亡非常有效，是设计新的抗癌药物的有希望的先导化合物。
We report herein a new class of small-molecule inhibitors of antiapoptotic Bcl-2 proteins. The most potent compound, 7, binds to Bcl-2, Bcl-xL, and Mcl-1 proteins with K-i of 110, 638, and 150 nM, respectively. Compound 7 is highly effective in induction of cell death in breast cancer cells with high levels of Bcl-2, Bcl-xL, and Mcl-1 proteins and represents a promising lead compound for the design of new anticancer drugs.