Design, synthesis, and studies of small molecule STAT3 inhibitors
Design, synthesis, and studies of small molecule STAT3 inhibitors
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DOI：
10.1016/j.bmcl.2007.10.031
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发表时间：
2008-01-01
影响因子：
2.7
通讯作者：
Li, Pui-Kai
中科院分区：
文献类型：
--
作者：
Bhasin, Deepak;Cisek, Katryna;Li, Pui-Kai
从我们的先导化合物STA21中合成了一系列小分子STAT3抑制剂，并对其进行了评价。这一系列中最有效的化合物，化合物1，表现出与STA21相同的抗增殖活性，对表达成分活性STAT3的前列腺癌细胞株。分子对接显示化合物1以类似于STAT21的方式与STAT3βSH2结构域结合。(C)2007爱思唯尔有限公司。保留所有权利。
A series of small molecule STAT3 inhibitors originally derived from our lead compound STA 21 were synthesized and evaluated. The most potent compound in this series, compound 1, exhibited the same anti-proliferative activities as STA 21 against prostate cancer cell lines that express constitutively active STAT3. Molecular docking showed compound 1 bound to the STAT3 beta SH2 domain in a similar manner as STA 21. (C) 2007 Elsevier Ltd. All rights reserved.