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

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

Affiliation

  • 1 Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd., Mason, OH 45040, USA. Mark.Sabat@Takedasd.com
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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