Head-to-head bisbenzazole derivatives as antiproliferative agents: design, synthesis, in vitro activity, and SAR analysis

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dc.authoridHAJ ERSAN, RONAK/0000-0001-6651-5910
dc.contributor.authorErsan, Ronak Haj
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorErtan-Bolelli, Tugba
dc.contributor.authorDuran, Nizami
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2024-09-18T20:04:31Z
dc.date.available2024-09-18T20:04:31Z
dc.date.issued2021
dc.departmentHatay Mustafa Kemal Üniversitesien_US
dc.description.abstractIn the present work, a series of bisbenzazole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of these compounds was investigated using MTT assay. Bisbenzazole derivatives showed significant antiproliferative activity against all the four tested cancer cell lines. Among the various bisbenzazole derivatives, bisbenzoxazole derivatives exhibited the most promising anticancer activity followed by bisbenzimidazole and bisbenzothiazole derivatives. All the derivatives were found to be less toxic as compared to methotrexate (positive control) in normal human cells, indicating selective and efficient antiproliferative activity of these bisbenzazole derivatives. The structure-activity relationships of heteroaromatic systems and linkers present in bisbenzazole derivatives were analyzed in detail. In silico ADMET prediction revealed that bisbenzazole is a drug-like small molecule with a favorable safety profile. Compound31is a potential antiproliferative hit compound that exhibits unique cytotoxic activity distinct from methotrexate. [GRAPHICS]en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [115S190]; Mersin University [2018-1-TP3-2911]en_US
dc.description.sponsorshipWe thank the Scientific and Technological Research Council of Turkey (TUBITAK, Grant Number: 115S190) and Mersin University (Project Number: 2018-1-TP3-2911) for their financial support.en_US
dc.identifier.doi10.1007/s11030-020-10115-0
dc.identifier.endpage2259en_US
dc.identifier.issn1381-1991
dc.identifier.issn1573-501X
dc.identifier.issue4en_US
dc.identifier.pmid32556804en_US
dc.identifier.scopus2-s2.0-85086647957en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage2247en_US
dc.identifier.urihttps://doi.org/10.1007/s11030-020-10115-0
dc.identifier.urihttps://hdl.handle.net/20.500.12483/8228
dc.identifier.volume25en_US
dc.identifier.wosWOS:000541187100001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofMolecular Diversityen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBisbenzimidazoleen_US
dc.subjectBisbenzoxazoleen_US
dc.subjectBisbenzothiazoleen_US
dc.subjectAntiproliferative activityen_US
dc.subjectSARen_US
dc.subjectADMETen_US
dc.titleHead-to-head bisbenzazole derivatives as antiproliferative agents: design, synthesis, in vitro activity, and SAR analysisen_US
dc.typeArticleen_US

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