The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck)

  • Bioorg Med Chem Lett. 2006 Dec 1;16(23):5973-7. doi: 10.1016/j.bmcl.2006.08.132.
Mark Sabat  1 ,  John C VanRens ,  Matthew J Laufersweiler ,  Todd A Brugel ,  Jennifer Maier ,  Adam Golebiowski ,  Biswanath De ,  Vijayasurian Easwaran ,  Lily C Hsieh ,  Richard L Walter ,  Marlene J Mekel ,  Artem Evdokimov ,  Michael J Janusz
Affiliations
  • 1. Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd., Mason, OH 45040, USA. [email protected]
PMID: 16997556 DOI: 10.1016/j.bmcl.2006.08.132
Abstract

This communication details the synthesis, biological activity, and binding mode of a novel class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase and a representative analog was co-crystallized with Hck (a structurally related member of the Src family kinases).

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