| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372004 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release.
Graphical abstractCompound 4 was found to be a potent inhibitor of Lck activity (IC50 = 0.1 nM) and cellular IL2 release (IC50 = 8 nM).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Julianne A. Hunt, Richard T. Beresis, Joung L. Goulet, Mark A. Holmes, Xinfang J. Hong, Ernest Kovacs, Sander G. Mills, Rowena D. Ruzek, Frederick Wong, Jeffrey D. Hermes, Young-Whan Park, Scott P. Salowe, Lisa M. Sonatore, Lin Wu, Andrea Woods,