Biological activity and ADME/Tox prediction of some 2-substituted benzoxazole derivatives

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dc.contributor.authorFoto, Fatma Zilifdar
dc.contributor.authorFoto, Egemen
dc.contributor.authorErtan-Bolelli, Tugba
dc.contributor.authorYildiz, Ilkay
dc.date.accessioned2024-02-23T14:02:14Z
dc.date.available2024-02-23T14:02:14Z
dc.date.issued2022
dc.departmentNEÜen_US
dc.description.abstractIn this study, we mainly focused on some in vitro biological activities of a series of (5 or 6)-amino-2- (substituted phenyl and benzyl) benzoxazole derivatives. For this purpose, we tested cytotoxic and genotoxic activities of them on cancer cell lines and their topoisomerase inhibitory activities. We also tested their cytotoxic and genotoxic activities on non-cancerous cells (L929) and their mutagenic activities by Ames test to evaluate their effects on healthy cells. Only TD5 was found cytotoxic on all the tested cancer cell lines and did not exhibit either cytotoxic or genotoxic activities against healthy cells, whereas TD1, TD2, TD3 and TD7 were more cytotoxic against only HeLa cells. Only TD4 was found as mutagenic derivative. None of the compounds had any topoisomerase inhibitory activities nevertheless some of them caused inhibition of topoisomerase II activity. Additionally, we used an in silico model to predict the drug-like properties of them to evaluate their bioavailability to the QikProp Properties Predictions. All the calculated properties were found in a permissible range. According to the data obtained from biological activity studies, it can be concluded that the methylene bridge at the position 2 of benzoxazole ring decreases cytotoxic activity on cancer cells and inhibitory activity on DNA topoisomerases.en_US
dc.description.sponsorshipAnkara University Research Fund [18H0237001]; Hacettepe University Scientific Research Projects Coordination Unit [FHD-2019-17892]en_US
dc.description.sponsorshipAcknowledgements This study was supported by Ankara University Research Fund (Grant no. 18H0237001) and Hacettepe University Scientific Research Projects Coordination Unit (Project number. FHD-2019-17892) .en_US
dc.identifier.doi10.1016/j.bioorg.2022.105756
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid35381557en_US
dc.identifier.scopus2-s2.0-85127355987en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2022.105756
dc.identifier.urihttps://hdl.handle.net/20.500.12452/11639
dc.identifier.volume123en_US
dc.identifier.wosWOS:000792922300008en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBenzoxazoleen_US
dc.subjectAmes Testen_US
dc.subjectComet Assayen_US
dc.subjectAdmeen_US
dc.subjectToxen_US
dc.subjectAntiproliferative Activityen_US
dc.subjectTopoisomeraseen_US
dc.titleBiological activity and ADME/Tox prediction of some 2-substituted benzoxazole derivativesen_US
dc.typeArticleen_US

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