Disubstituted pyrimidines as Lck inhibitors

JA Hunt, RT Beresis, JL Goulet, MA Holmes…

Index: Hunt, Julianne A.; Beresis, Richard T.; Goulet, Joung L.; Holmes, Mark A.; Hong, Xinfang J.; Kovacs, Ernest; Mills, Sander G.; Ruzek, Rowena D.; Wong, Frederick; Hermes, Jeffrey D.; Park, Young-Whan; Salowe, Scott P.; Sonatore, Lisa M.; Wu, Lin; Woods, Andrea; Zaller, Dennis M.; Sinclair, Peter J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 18 p. 5440 - 5443

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Citation Number: 4

Abstract

We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release.

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