Exploring the newer oxadiazoles as real inhibitors of human SIRT2 in hepatocellular cancer cells

Dukanya and Shanmugam, Muthu K. and Rangappa, Shobith and Metri, Prashant K. and Mohan, Surender and Basappa and Rangappa, Kanchugarakoppal S. (2020) Exploring the newer oxadiazoles as real inhibitors of human SIRT2 in hepatocellular cancer cells. Bioorganic & Medicinal Chemistry Letters, 30 (16). ISSN 1464-3405

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Abstract

A novel series of indazole tethered oxadiazoles (OTDs) derivatives were synthesized, characterized and screened for their anti-proliferative activity against hepatocellular carcinoma (HCC) cells. OTDs structure was further confirmed by Single-crystal X-ray diffraction studies. Among the tested OTDs, compound 2-(4-methoxyphenyl)-5-(1-methyl-1H-indazol-3-yl)-1,3,4 oxadiazole was found to inhibit the catalytical activity of SIRT2 and brings about apoptosis as shown by western blot analysis and flow cytometry data. Also, the tested OTDs were found to interact with the active site of human SIRT2 in silico but not with the cavity of co-crystal ligand 5-(3- hydroxypropyl)-3-(4-chlorophenyl)-1,2,4-oxadiazole, which indicate that these OTDs has potential in the development of SIRT2 inhibitors in liver cancer models.

Item Type: Article
Uncontrolled Keywords: SIRT2; Indazole; Oxadiazole; HCC; Drug-discovery
Subjects: C Chemical Science > Organic Chemistry
Divisions: Department of > Organic Chemistry
Depositing User: Mr Umendra uom
Date Deposited: 05 Mar 2021 06:02
Last Modified: 05 Mar 2021 06:02
URI: http://eprints.uni-mysore.ac.in/id/eprint/15531

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