Design and synthesis of novel 1,2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors
Design and synthesis of novel 1,2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors
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作为 PTP1B 抑制剂的新型 1,2-二硫杂环戊烷-4-基苯甲酸酯衍生物的设计与合成
DOI：
10.1016/j.bmcl.2015.03.060
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发表时间：
2015-05-15
影响因子：
2.7
通讯作者：
Guo, Yue-Wei
中科院分区：
文献类型：
--
作者：
Chen, Jing;Gao, Li-Xin;Guo, Yue-Wei
A series of novel 1,2-dithiolan-4-yl benzoate compounds were synthesized and evaluated for in vitro PTP1B inhibitory activity. Some derivatives exhibited improved PTP1B inhibitory activity and selectivity compared to hit 6a, a compound from in-house library screening inspired by marine cyclic disulfide. The preliminary SAR analysis with assistance of molecular modeling approach revealed 6j (IC50 = 0.59 mu M) as the most potent PTP1B inhibitor among all derivatives. (C) 2015 Elsevier Ltd. All rights reserved.
