The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).
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Sabat M, VanRens JC, Laufersweiler MJ, Brugel TA, Maier J, Golebiowski A, De B, Easwaran V, Hsieh LC, Walter RL, Mekel MJ, Evdokimov A, Janusz MJ
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. Epub 2006 Sep 25.
- PubMed ID
- 16997556 [ View in PubMed]
- 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).