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Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II |
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| Authors: | Guobao Zhang Pingda Ren Nathanael S Gray Taebo Sim Xia Wang Yi Liu Jianwei Che Weitong Dong Shin-Shay Tian Mark L Sandberg Tracy A Spalding Russell Romeo Maya Iskandar Zhiliang Wang H Martin Seidel Donald S Karanewsky Yun He |
| Institution: | Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA |
| Abstract: | A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src-family kinases (SFKs). These type II inhibitors were optimized using a cellular Lck-dependent proliferation assay and are capable of inhibiting Lck at single-digit nanomolar concentrations. This scaffold is likely to serve a valuable template for developing potent inhibitors of a number of SFKs. |
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