Download MendeleyDiscovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.
Labroli, M., Paruch, K., Dwyer, M.P., Alvarez, C., Keertikar, K., Poker, C., Rossman, R., Duca, J.S., Fischmann, T.O., Madison, V., Parry, D., Davis, N., Seghezzi, W., Wiswell, D., Guzi, T.J.(2011) Bioorg Med Chem Lett 21: 471-474
- PubMed: 21094607
- DOI: https://doi.org/10.1016/j.bmcl.2010.10.114
- Primary Citation of Related Structures:
3OT3 - PubMed 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 C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors.
Organizational Affiliation:
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States. marc.labroli@merck.com
