Discovery of pyrazolo [1, 5-a] pyrimidine-based CHK1 inhibitors: A template-based approach—Part 2

…, C Alvarez, K Keertikar, C Poker, R Rossman…

Index: Labroli, Marc; Paruch, Kamil; Dwyer, Michael P.; Alvarez, Carmen; Keertikar, Kartik; Poker, Cory; Rossman, Randall; Duca, Jose S.; Fischmann, Thierry O.; Madison, Vincent; Parry, David; Davis, Nicole; Seghezzi, Wolfgang; Wiswell, Derek; Guzi, Timothy J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 467 - 470

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Citation Number: 28

Abstract

Previous efforts by our group have established pyrazolo [1, 5-a] pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo [1, 5-a] pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1, 5-a] pyrimidine core at the C5 and ...