Synthesis and Biological Evaluation of New Quinoline-Based Thiazolyl Hydrazone Derivatives as Potent Antifungal and Anticancer Agents

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dc.contributor.authorErguc, Ali
dc.contributor.authorAltintop, Mehlika Dilek
dc.contributor.authorAtli, Ozlem
dc.contributor.authorSever, Belgin
dc.contributor.authorIscan, Gokalp
dc.contributor.authorGormus, Gozde
dc.contributor.authorOzdemir, Ahmet
dc.date.accessioned2019-10-27T10:46:43Z
dc.date.available2019-10-27T10:46:43Z
dc.date.issued2018
dc.departmentEge Üniversitesien_US
dc.description.abstractBackground: In medicinal chemistry, thiazoles have gained great importance in anti-fungal and anticancer drug design and development. Objectives: The aim of this study was to synthesize new quinoline-based thiazolyl hydrazone derivatives and evaluate their anticandidal and anticancer effects. Methods: New thiazolyl hydrazone derivatives were evaluated for their anticandidal effects using disc diffusion method. Ames MPF assay was carried out to determine the genotoxicity of the most effective antifungal derivative. MTT assay was also performed to assess the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, MCF7 human breast adenocarcinoma and NIH/3T3 mouse embryonic fibroblast (healthy) cell lines. Results: 4-(4-Fluorophenyl)-2-(2-((quinolin-4-yl) methylene) hydrazinyl) thiazole (4) showed antifungal activity against Candida albicans and Candida krusei in the concentration of 1 mg/mL. In MTT and Ames MPF tests, it was determined that compound 4 did not show cytotoxic and genotoxic effects. MTT assay indicated that 4-(naphthalen-2-yl)-2-(2-((quinolin-4-yl) methylene) hydrazinyl) thiazole (10) showed more selective anticancer activity than cisplatin against A549 and MCF-7 cell lines. Besides, 4-(4-chlorophenyl)-2-(2-((quinolin-4-yl) methylene) hydrazinyl) thiazole (5) exhibited more selective anticancer activity than cisplatin against HepG2 cell line. Conclusion: Due to their high selectivity index, these compounds are considered as candidate compounds to participate in further research.en_US
dc.identifier.doi10.2174/1570180814666171003145227
dc.identifier.endpage202en_US
dc.identifier.issn1570-1808
dc.identifier.issn1875-628X
dc.identifier.issn1570-1808en_US
dc.identifier.issn1875-628Xen_US
dc.identifier.issue2en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage193en_US
dc.identifier.urihttps://doi.org/10.2174/1570180814666171003145227
dc.identifier.urihttps://hdl.handle.net/11454/31337
dc.identifier.volume15en_US
dc.identifier.wosWOS:000423791300010en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.language.isoenen_US
dc.publisherBentham Science Publ Ltden_US
dc.relation.ispartofLetters in Drug Design & Discoveryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectThiazoleen_US
dc.subjecthydrazoneen_US
dc.subjectquinolineen_US
dc.subjectanticancer activityen_US
dc.subjectanticandidal activityen_US
dc.subjectgenotoxicityen_US
dc.titleSynthesis and Biological Evaluation of New Quinoline-Based Thiazolyl Hydrazone Derivatives as Potent Antifungal and Anticancer Agentsen_US
dc.typeArticleen_US

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