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6. Identification and biological evaluation of novel benzothiazole derivatives bearing a pyridine-semicarbazone moiety as apoptosis inducers via activation of procaspase-3 to caspase-3

Author

Yali Gao, Jiaan Liu, Ni Xin, Cui-Fang Wang, Junjie Ma, Yu Wang, Huang Kun, and Chen Roufen

Subjects
Pharmacology, Chemistry, Organic Chemistry, Pharmaceutical Science, Caspase 3, Biochemistry, In vitro, chemistry.chemical_compound, Benzothiazole, In vivo, Apoptosis, Drug Discovery, Cancer cell, Molecular Medicine, Moiety, Semicarbazone
Abstract

Three series of compounds were designed, synthesized and evaluated for their in vitro anticancer activity against a procaspase-3 over-expression cancer cell line (U937) and a procaspase-3 no-expression cancer cell line (MCF-7) to rule out off-target effects. Biological evaluation led to the identification of a series of benzothiazole derivatives bearing a pyridine-semicarbazone moiety, 8j and 8k, with promising anticancer activity and remarkable selectivity. Further mechanism studies revealed that compounds 8j and 8k could induce apoptosis of cancer cells by activating procaspase-3 to caspase-3, and compound 8k exhibited the strongest procaspase-3 activation activity. Structure–activity relationships (SARs) revealed that the presence of benzothiazole and an N,N,O-donor set is crucial for the anticancer activity and selectivity, and reducing the electron density of the N,N,O-donor set results in a dramatic decline in the anticancer activity and selectivity. Furthermore, toxicity evaluation (zebrafish) in vivo and metabolic stability studies (human, rat and mouse liver microsomes) were performed to provide reliable guidance for further PK/PD studies in vivo.

Published
2019

8. Advances in research on 3C-like protease (3CL pro ) inhibitors against SARS-CoV-2 since 2020.

Author

Chen R, Gao Y, Liu H, Li H, Chen W, and Ma J

Abstract

COVID-19 caused by SARS-CoV-2 in late 2019 is still threatening global human health. Although some vaccines and drugs are available in the market, controlling the spread of the SARS-CoV-2 virus remains a huge challenge. 3C-like protease (3CL pro ) is a highly conserved key protease for SARS-CoV-2 replication, and no relevant homologous protein with a similar cleavage site to 3CL pro has been identified in humans, highlighting that development of 3CL pro inhibitors exhibits great promise for treatment of COVID-19. In this review, the authors describe the structure and function of 3CL pro . To better understand the characteristics of SARS-CoV-2 3CL pro inhibitors, the SARS-CoV-2 3CL pro inhibitors reported since 2020 are classified into peptidomimetic covalent inhibitors, non-peptidomimetic covalent inhibitors and non-covalent small molecule inhibitors, and the representative inhibitors, their biological activities and binding models are highlighted. Collectively, we hope that all the information presented here will provide new insights into the design and development of more effective 3CL pro inhibitors against SARS-CoV-2 as novel anti-coronavirus drugs., Competing Interests: There is no conflict of interest to declare., (This journal is © The Royal Society of Chemistry.)

Published
2022
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