PT  - JOURNAL ARTICLE
AU  - ARIANNA GELAIN
AU  - MATTEO MORI
AU  - FIORELLA MENEGHETTI
AU  - FEDERICA PORTA
AU  - LIVIA BASILE
AU  - GAETANO MARVERTI
AU  - AKIRA ASAI
AU  - MARIAFRANCESCA HYERACI
AU  - AÍDA NELLY GARCÍA-ARGÁEZ
AU  - LISA DALLA VIA
AU  - SALVATORE GUCCIONE
AU  - STEFANIA VILLA
TI  - Exploring the Biological Activity of a Library of 1,2,5-Oxadiazole Derivatives Endowed With Antiproliferative Activity
AID  - 10.21873/anticanres.13089
DP  - 2019 Jan 01
TA  - Anticancer Research
PG  - 135--144
VI  - 39
IP  - 1
4099  - http://ar.iiarjournals.org/content/39/1/135.short
4100  - http://ar.iiarjournals.org/content/39/1/135.full
SO  - Anticancer Res2019 Jan 01; 39
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.