Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591919 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
Drug design efforts in the emerging 2-aminothiazole-4-carboxamide class of CHK1 inhibitors have uncovered specific combinations of key substructures within the molecule; resulting in significant improvements in cell-based activity while retaining a greater than one hundred-fold selectivity against CDK2. The X-ray crystal structure of a complex between compound 39 and the CHK1 protein detailing a 'U-shaped' topology and key interactions with the protein surface at the ATP site is also reported.
Related Topics
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Authors
Xiaohua Huang, Cliff C. Cheng, Thierry O. Fischmann, José S. Duca, Matthew Richards, Praveen K. Tadikonda, Panduranga Adulla Reddy, Lianyun Zhao, M. Arshad Siddiqui, David Parry, Nicole Davis, Wolfgang Seghezzi, Derek Wiswell, Gerald W. Jr.,