De novo design, synthesis and biological evaluation of 1, 4-dihydroquinolin-4-ones and 1, 2, 3, 4-tetrahydroquinazolin-4-ones as potent kinesin spindle protein (KSP) …

C Jiang, L Yang, WT Wu, QL Guo, QD You

Index: Jiang, Cheng; Yang, Lei; Wu, Wu-Tong; Guo, Qing-Long; You, Qi-Dong Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5612 - 5627

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Citation Number: 21

Abstract

Kinesin spindle protein (KSP) inhibitors are a promising class of anticancer agents that cause mitotic arrest in cells from a failure to form functional bipolar mitotic spindles. Here, we report the design, synthesis and biological evaluation of a novel series of 1, 4- dihydroquinolin-4-ones and 1, 2, 3, 4-tetrahydroquinazolin-4-ones using de novo design method. The synthesized compound was evaluated and proved to have potent inhibitory ...