Disubstituted pyrimidines as Lck inhibitors
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- 作者：Julianne A. Hunt ; Richard T. Beresis ; Joung L. Goulet ; Mark A. Holmes ; Xinfang J. Hong ; Ernest Kovacs ; S ; er G. Mills ; Rowena D. Ruzek ; Frederick Wong ; Jeffrey D. Hermes ; Young-Whan Park ; Scott P. Salo
- 关键词：Lck ; Src ; Protein tyrosine kinase ; Autoimmune disease ; Rheumatoid arthritis ; Pyrimidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 September 2009
- 年：2009
- 卷：19
- 期：18
- 页码：5440-5443
- 全文大小：462 K
文摘
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.