Design, synthesis and bioevaluation of dihydropyrazolo [3, 4-b] pyridine and benzo [4, 5] imidazo [1, 2-a] pyrimidine compounds as dual KSP and Aurora-A kinase …

R Fu, Q You, L Yang, W Wu, C Jiang, X Xu

Index: Fu, Rong-Geng; You, Qi-Dong; Yang, Lei; Wu, Wu-Tong; Jiang, Cheng; Xu, Xiao-Li Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 22 p. 8035 - 8043

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Citation Number: 25

Abstract

Four series of dihydropyrazolo [3, 4-b] pyridines and benzo [4, 5] imidazo [1, 2-a] pyrimidines were designed and synthesized as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents by introducing some fragments of Aurora-A kinase inhibitors into our KSP inhibitor CPUYL064. A total of 19 target compounds were evaluated by two related enzyme inhibition assays and a cytotoxicity assay in vitro. The results showed that some target compounds ...