Title of article
Discovery and structure–activity relationships of novel sulfonamides as potent PTP1B inhibitors
Author/Authors
Christopher P. Holmes، نويسنده , , Xianfeng Li، نويسنده , , Yijun Pan، نويسنده , , Caiding Xu، نويسنده , , Ashok Bhandari، نويسنده , , Claire M. Moody، نويسنده , , Joy A. Miguel، نويسنده , , Steven W. Ferla، نويسنده , , M. Nuria De Francisco، نويسنده , , Brian T. Frederick، نويسنده , , Siqun Zhou، نويسنده , , Natalie Macher، نويسنده , , Larry Jang، نويسنده , , Jennifer D. Irvine، نويسنده , , J. Russell Grove، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
4336
To page
4341
Abstract
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 Ki 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.
Keywords
sulfonamides , PTP1B inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795988
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