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Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1 |
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| Authors: | Dwyer Michael P Paruch Kamil Labroli Marc Alvarez Carmen Keertikar Kerry M Poker Cory Rossman Randall Fischmann Thierry O Duca Jose S Madison Vincent Parry David Davis Nicole Seghezzi Wolfgang Wiswell Derek Guzi Timothy J |
| Institution: | a Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA b Merck Research Laboratories, 901 California Avenue, Palo Alto, CA 94304, USA c Merck Research Laboratories, 320 Bent St., Cambridge, MA 02141, USA |
| Abstract: | The synthesis and hit-to-lead SAR development of a pyrazolo1,5-a]pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed. |
| Keywords: | Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template |
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