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

Full Text: HTML

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 ...

~99%

~99%

~44%

~99%

~51%

~60%

~97%

~99%

~99%

~98%

~99%

~99%

~99%

~44%

~99%

~99%

~98%

~99%

~49%

~42%

Reactivity of carbamoyl radicals. A new, general, convenient...

[Minisci, Francesco; Fontana, Francesca; Coppa, Fausta; Yan, Yong Ming Journal of Organic Chemistry, 1995 , vol. 60, # 17 p. 5430 - 5433]

Organometallic chemistry and catalysis on gold metal surface...

[Journal of Organometallic Chemistry, , vol. 693, # 5 p. 847 - 856]

Matrix-IR Spectroscopic Investigations of the Thermolysis an...

[Paraskewas, Spyridon M.; Danopoulos, Andreas A. Synthesis, 1983 , # 8 p. 638 - 640]

Selective muscarinic antagonists. II. Synthesis and antimusc...

[Chemical and Pharmaceutical Bulletin, , vol. 46, # 8 p. 1286 - 1294]