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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 C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors. Copyright © 2010 Elsevier Ltd. All rights reserved.

Citation

Marc Labroli, Kamil Paruch, Michael P Dwyer, Carmen Alvarez, Kartik Keertikar, Cory Poker, Randall Rossman, Jose S Duca, Thierry O Fischmann, 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 2. Bioorganic & medicinal chemistry letters. 2011 Jan 1;21(1):471-4

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PMID: 21094607

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