期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 6, 页码 1348-1355出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.01.025
关键词
STAT3; Inhibitor; SARs; SH2; Small organic molecule; Molecular docking
资金
- Miami University
- AACR-Pancreatic Cancer Action Network Innovation grant
Inhibition of the signaling pathways of signal transducer and activator of transcription 3 (STAT 3) has shown to be a promising strategy to combat cancer. In this paper we report the design, synthesis and evaluation of a novel class of small molecule inhibitors, that is, XZH-5 and its analogues, as promising leads for further development of STAT3 inhibitors. Preliminary SARs was established for XZH-5 and its derivatives; and the binding modes were predicted by molecular docking. Lead compounds with IC50 as low as 6.5 mu M in breast cancer cell lines and 7.6 mu M in pancreatic cancer cell lines were identified. (C) 2015 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据