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Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR) |
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| Authors: | Sreekanth A. Ramachandran Pradeep S. Jadhavar Manvendra P. Singh Ankesh Sharma Gaurav N. Bagle Kevin P. Quinn Po-yin Wong Andrew A. Protter Roopa Rai Son M. Pham Jeffrey N. Lindquist |
| Affiliation: | 1. Integral BioSciences, Pvt. Ltd., C-64, Hosiery Complex Phase II Extension, Noida, Uttar Pradesh, 201306, India;2. Medivation, Now Pfizer Inc., 525 Market Street, 36th Floor, San Francisco, CA 94105, United States;3. Current address: Palo Alto Pharmaceutical Consulting Service, United States |
| Abstract: | The ATR pathway is a critical mediator of the replication stress response in cells. In aberrantly proliferating cancer cells, this pathway can help maintain sufficient genomic integrity for cancer cell progression. Herein we describe the discovery of 19, a pyrazolopyrimidine-containing inhibitor of ATR via a strategic repurposing of compounds targeting PI3K. |
| Keywords: | ATR Pyrazolopyrimidine DNA damage PI3K HTS |
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