Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I)

…, D Aivazian, D Marcotte, G Xiao, JY Le Brazidec…

文献索引：Zhang, Lin; Fan, Junhua; Chong, Jer-Hong; Cesena, Angela; Tam, Betty Y.Y.; Gilson, Charles; Boykin, Christina; Wang, Deping; Aivazian, Dikran; Marcotte, Doug; Xiao, Guangqing; Le Brazidec, Jean-Yves; Piao, Jinhua; Lundgren, Karen; Hong, Kevin; Vu, Khang; Nguyen, Khanh; Gan, Liang-Shang; Silvian, Laura; Ling, Leona; Teng, Min; Reff, Mitchell; Takeda, Nicole; Timple, Noel; Wang, Qin; Morena, Ron; Khan, Samina; Zhao, Shuo; Li, Tony; Lee, Wen-Cherng; Taveras, Arthur G.; Chao, Jianhua Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5633 - 5637

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被引用次数: 6

摘要

A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development has led to the discovery of potent inhibitors with single digit nM IC50s towards both AKA and CDK1. An exemplary compound 1a has demonstrated good efficacy in an HCT116 colon cancer ...