Publication details
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.
| Authors | |
|---|---|
| Year of publication | 2011 |
| Type | Article in Periodical |
| Magazine / Source | Bioorganic & Medicinal Chemistry Letters |
| MU Faculty or unit | |
| Citation | |
| Doi | http://dx.doi.org/10.1016/j.bmcl.2010.10.113 |
| Field | Organic chemistry |
| Keywords | Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template |
| Description | 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. |