Discovery of pyrazolo [1, 5-a] pyrimidine-based CHK1 inhibitors: A template-based approach—Part 1

…, K Paruch, M Labroli, C Alvarez, KM Keertikar…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 471 - 474

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Citation Number: 32

Abstract

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.