Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I
Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I
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DOI:
10.1016/j.bmcl.2008.08.104
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发表时间:
2008-10-15
影响因子:
2.7
通讯作者:
He, Yun
中科院分区:
文献类型:
--
作者:
Zhang, Guobao;Ren, Pingda;He, Yun
A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues for SAR studies. A number of these 4-amino-6-benzimidazole-pyrimidines exhibited single-digit nanomolar IC(50)s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.