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Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents: parallel synthesis for lead optimization of amide region. 2005
Ariamala Gopalsamy, and
Hui Yang, and
John W Ellingboe, and
Hwei-Ru Tsou, and
Nan Zhang, and
Erick Honores, and
Dennis Powell, and
Miriam Miranda, and
John P McGinnis, and
Sridhar K Rabindran
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. gopalsa@wyeth.com
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.
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