Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR)

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• 作者：Sreekanth A. Ramachandran^a ; Pradeep S. Jadhavar^a ; Manvendra P. Singh^a ; Ankesh Sharma^a ; Gaurav N. Bagle^a ; Kevin P. Quinn^b ; Po-yin Wong^b ; Andrew A. Protter^b ; ^c ; Roopa Rai^b ; Son M. Pham^b ; ; Jeffrey N. Lindquist^b ; ^{pham.sm@gmail.com}
• 关键词：ATR ; Pyrazolopyrimidine ; DNA damage ; PI3K ; HTS
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：750-754
• 全文大小：1000 K
• 卷排序：27

文摘

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.