Design, synthesis and evaluation of 1, 2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors

D Liu, Z Tian, Z Yan, L Wu, Y Ma, Q Wang, W Liu…

Index: Liu, Dazhi; Tian, Zhen; Yan, Zhihui; Wu, Lixin; Ma, Yan; Wang, Quan; Liu, Wei; Zhou, Honggang; Yang, Cheng Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 2960 - 2967

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Citation Number: 22

Abstract

A number of 1, 2-benzisothiazol-3-one derivatives were prepared through structural modification of the original compound from high-throughput screening. Some analogues (eg, 6b, 6r, 6s and 6w) were identified as novel and potent caspase inhibitors with IC50 of nanomolar. Structure–activity relationship (SAR) studies for caspase-3 inhibition were evaluated in vitro. Molecular modeling studies provided further insight into the interaction ...

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