Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors
Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors
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DOI：
10.1016/j.bmcl.2005.06.061
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发表时间：
2005-10-01
影响因子：
2.7
通讯作者：
Grove, JR
中科院分区：
文献类型：
--
作者：
Holmes, CP;Li, XF;Grove, JR
A series of novel sulfonamides containing a single difluoromethylene-phosphonate group were discovered to be potent inhibitors of protein tyrosine phosphatase 1B. Structure-activity relationships around the scaffold were investigated, leading to the identification of compounds with IC50 or K-i values in the low nanomolar range. These sulfonamide-based inhibitors exhibit 100 and 30 times higher inhibitory activity than the corresponding tertiary amines and carboxamides, respectively. (c) 2005 Elsevier Ltd. All rights reserved.
