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Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I |
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| Authors: | Zhang Guobao Ren Pingda Gray Nathanael S Sim Taebo Liu Yi Wang Xia Che Jianwei Tian Shin-Shay Sandberg Mark L Spalding Tracy A Romeo Russell Iskandar Maya Chow Donald Martin Seidel H Karanewsky Donald S He Yun |
| Institution: | Genomics Institute of the Novartis Research Foundation (GNF), Medicinal Chemistry, 10715 John Jay Hopkins Drive, San Diego, CA 92121, USA. gzhang@gnf.org |
| Abstract: | 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. |
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