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 ,
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.
