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

…, J Maier, A Golebiowski, B De, V Easwaran…

Index: Sabat, Mark; VanRens, John C.; Laufersweiler, Matthew J.; Brugel, Todd A.; Maier, Jennifer; Golebiowski, Adam; De, Biswanath; Easwaran, Vijayasurian; Hsieh, Lily C.; Walter, Richard L.; Mekel, Marlene J.; Evdokimov, Artem; Janusz, Michael J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 5973 - 5977

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Citation Number: 44

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).