Download MendeleyDiscovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 1.
Dwyer, M.P., Paruch, K., Labroli, M., Alvarez, C., Keertikar, K.M., Poker, C., Rossman, R., Fischmann, T.O., Duca, J.S., Madison, V., Parry, D., Davis, N., Seghezzi, W., Wiswell, D., Guzi, T.J.(2011) Bioorg Med Chem Lett 21: 467-470
- PubMed: 21094608
- DOI: https://doi.org/10.1016/j.bmcl.2010.10.113
- Primary Citation of Related Structures:
3OT8 - PubMed 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.
Organizational Affiliation:
Merck Research Laboratories, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, USA. [email protected]
