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

Autor: Sabat M; Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd., Mason, OH 45040, USA. Mark.Sabat@Takedasd.com , VanRens JC, Laufersweiler MJ, Brugel TA, Maier J, Golebiowski A, De B, Easwaran V, Hsieh LC, Walter RL, Mekel MJ, Evdokimov A, Janusz MJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Dec 01; Vol. 16 (23), pp. 5973-7. Date of Electronic Publication: 2006 Sep 25.
DOI: 10.1016/j.bmcl.2006.08.132
Abstrakt: 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).
Databáze: MEDLINE