Design, synthesis, and biological evaluation of isoquinoline-1, 3, 4-trione derivatives as potent caspase-3 inhibitors

YH Chen, YH Zhang, HJ Zhang, DZ Liu…

Index: Chen, Yi-Hua; Zhang, Ya-Hui; Zhang, Hua-Jie; Liu, Da-Zhi; Gu, Min; Li, Jing-Ya; Wu, Fang; Zhu, Xing-Zu; Li, Jia; Nan, Fa-Jun Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1613 - 1623

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Citation Number: 94

Abstract

A series of isoquinoline-1, 3, 4-trione derivatives were identified as novel and potent inhibitors of caspase-3 through structural modification of the original compound from high- throughput screening. Various analogues (2, 6, 9, 13, and 14) were synthesized and identified as caspase inhibitors, and the introduction of a 6-N-acyl group (compound 13) greatly improved their activity. Some of them showed low nanomolar potency against ...