Abstract:
BACKGROUND/AIM:The identification of a series of oxadiazole-based compounds, as promising antiproliferative agents, has been previously reported. The aim of this study was to explore the SAR of newly-synthesized oxadiazole derivatives and identify their molecular targets. MATERIALS AND METHODS:A small library of 1,2,5-oxadiazole derivatives was synthetized and their antiproliferative activity was tested by the MTT assay. Their interaction with topoisomerase I was evaluated and a molecular docking study was performed. RESULTS:Several candidates showed cytotoxicity towards two human tumor cell lines, HCT-116 (colorectal carcinoma) and HeLa (cervix adenocarcinoma). Some derivatives exhibited inhibitory effects on the catalytic activity of topoisomerase I and this effect was supported by docking studies. CONCLUSION:The enzyme inhibition results, although not directly related to cytotoxicity, suggest that a properly modified 1,2,5 oxadiazole scaffold could be considered for the development of new anti-topoisomerase agents.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Gelain A,Mori M,Meneghetti F,Porta F,Basile L,Marverti G,Asai A,Hyeraci M,García-Argáez AN,Via LD,Guccione S,Villa Sdoi
10.21873/anticanres.13089subject
Has Abstractpub_date
2019-01-01 00:00:00pages
135-144issue
1eissn
0250-7005issn
1791-7530pii
39/1/135journal_volume
39pub_type
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