Literature DB >> 18083554

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

Holly L Deak1, 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.   

Abstract

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.

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Year:  2007        PMID: 18083554     DOI: 10.1016/j.bmcl.2007.11.123

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Application of shape-based and pharmacophore-based in silico screens for identification of Type II protein kinase inhibitors.

Authors:  Daniel Mucs; Richard A Bryce; Pascal Bonnet
Journal:  J Comput Aided Mol Des       Date:  2011-06-17       Impact factor: 3.686

  1 in total

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