Gopalsamy Ariamala, Yang Hui, Ellingboe John W, Tsou Hwei-Ru, Zhang Nan, Honores Erick, Powell Dennis, Miranda Miriam, McGinnis John P, Rabindran Sridhar K
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA.
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1591-4. doi: 10.1016/j.bmcl.2005.01.066.
A novel series of p21 chemoselective agents containing a pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides were identified by high throughput screening. Optimization of the amide region by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described. The isopropyl carbamate derivative 34 was identified as a highly chemoselective agent displaying a potency of 51 nM in the p21 deficient cell line.
