N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.

N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.

Bioorganic & medicinal chemistry letters (2007-12-18)

Holly L Deak, John R Newcomb, Joseph J Nunes, Christina Boucher, Alan C Cheng, Erin F DiMauro, Linda F Epstein, Paul Gallant, Brian L Hodous, Xin Huang, Josie H Lee, Vinod F Patel, Stephen Schneider, Susan M Turci, Xiaotian Zhu

PMID18083554

ABSTRAKT

N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, structure-activity relationships, and the synthesis of these inhibitors are reported herein.