• Bioorg. Med. Chem. Lett. · Sep 2011

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

    • Lin Zhang, Junhua Fan, Jer-Hong Chong, Angela Cesena, Betty Y Y Tam, Charles Gilson, Christina Boykin, Deping Wang, Dikran Aivazian, Doug Marcotte, Guangqing Xiao, Jean-Yves Le Brazidec, Jinhua Piao, Karen Lundgren, Kevin Hong, Khang Vu, Khanh Nguyen, Liang-Shang Gan, Laura Silvian, Leona Ling, Min Teng, Mitchell Reff, Nicole Takeda, Noel Timple, Qin Wang, Ron Morena, Samina Khan, Shuo Zhao, Tony Li, Wen-Cherng Lee, Arthur G Taveras, and Jianhua Chao.
    • Biogen Idec, 5200 Research Place, San Diego, CA 92122, United States. lin.zhang.ge@sbcglobal.net
    • Bioorg. Med. Chem. Lett. 2011 Sep 15; 21 (18): 5633-7.

    AbstractA 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.Copyright © 2011 Elsevier Ltd. All rights reserved.

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