| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374890 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.
Graphical abstractROCK inhibitors have been developed from 2-chromanyl- and 2-carboxamido-benzothiazoles. SAR studies and lead optimizations are described, which result in novel ROCK-II inhibitors with sub-nanomolar IC50s and good kinase selectivity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yan Yin, Li Lin, Claudia Ruiz, Michael D. Cameron, Jennifer Pocas, Wayne Grant, Thomas Schröter, Weimin Chen, Derek Duckett, Stephan Schürer, Philip LoGrasso, Yangbo Feng,