| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373363 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.
Graphical abstractA novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Lianyun Zhao, Yingxin Zhang, Chaoyang Dai, Timothy Guzi, Derek Wiswell, Wolfgang Seghezzi, David Parry, Thierry Fischmann, M. Arshad Siddiqui,