Synthesis, SAR and biological evaluation of 1, 6-disubstituted-1H-pyrazolo [3, 4-d] pyrimidines as dual inhibitors of Aurora kinases and CDK1

…, B Tam, C Boykin, C Black, D Wang, G Claassen…

Index: Le Brazidec, Jean-Yves; Pasis, Angela; Tam, Betty; Boykin, Christina; Black, Cheryl; Wang, Deping; Claassen, Gisela; Chong, Jer-Hong; Chao, Jianhua; Fan, Junhua; Nguyen, Khanh; Silvian, Laura; Ling, Leona; Zhang, Lin; Choi, Michael; Teng, Min; Pathan, Nuzhat; Zhao, Shuo; Li, Tony; Taveras, Art Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 5 p. 2070 - 2074

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Citation Number: 18

Abstract

Since the early 2000s, the Aurora kinases have become major targets of oncology drug discovery particularly Aurora-A and Aurora-B kinases (AKA/AKB) for which the selective inhibition in cells lead to different phenotypes. In addition to targeting these Aurora kinases involved in mitosis, CDK1 has been added as a primary inhibition target in hopes of enhancing the cytotoxicity of our chemotypes harboring the pyrazolopyrimidine core. SAR ...