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Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I) |
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| Authors: | 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 |
| Affiliation: | Biogen Idec, 5200 Research Place, San Diego, CA 92122, United States. lin.zhang.ge@sbcglobal.net |
| Abstract: | 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 IC(50)s towards both AKA and CDK1. An exemplary compound 1a has demonstrated good efficacy in an HCT116 colon cancer xenograft model. |
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