Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Merck Research Laboratories, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, USA. michael.dwyer@merck.com

Bioorganic & medicinal chemistry letters 2011 Jan 1

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The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-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 pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed. Copyright © 2010 Elsevier Ltd. All rights reserved.

Citation

Michael P Dwyer, Kamil Paruch, Marc Labroli, Carmen Alvarez, Kerry M Keertikar, Cory Poker, Randall Rossman, Thierry O Fischmann, Jose S Duca, Vincent Madison, David Parry, Nicole Davis, Wolfgang Seghezzi, Derek Wiswell, Timothy J Guzi. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1. Bioorganic & medicinal chemistry letters. 2011 Jan 1;21(1):467-70