| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1364793 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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 IC50s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.
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, Yi Liu, Xia Wang, Jianwei Che, Shin-Shay Tian, Mark L. Sandberg, Tracy A. Spalding, Russell Romeo, Maya Iskandar, Donald Chow, H. Martin Seidel, Donald S. Karanewsky, Yun He,