RT Journal Article SR Electronic T1 Exploring the Biological Activity of a Library of 1,2,5-Oxadiazole Derivatives Endowed With Antiproliferative Activity JF Anticancer Research JO Anticancer Res FD International Institute of Anticancer Research SP 135 OP 144 DO 10.21873/anticanres.13089 VO 39 IS 1 A1 ARIANNA GELAIN A1 MATTEO MORI A1 FIORELLA MENEGHETTI A1 FEDERICA PORTA A1 LIVIA BASILE A1 GAETANO MARVERTI A1 AKIRA ASAI A1 MARIAFRANCESCA HYERACI A1 AÍDA NELLY GARCÍA-ARGÁEZ A1 LISA DALLA VIA A1 SALVATORE GUCCIONE A1 STEFANIA VILLA YR 2019 UL http://ar.iiarjournals.org/content/39/1/135.abstract AB 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.