| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374891 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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.
Graphical abstractA series of 4-amino-6-benzimidazole-pyrimidines were designed and synthesized as potent Lck inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,