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dc.contributor.authorCevik, Ulviye Acar
dc.contributor.authorSaglik, Begum N.
dc.contributor.authorOsmaniye, Derya
dc.contributor.authorLevent, Serkan
dc.contributor.authorCavusoglu, Betul Kaya
dc.contributor.authorKaraduman, Abdullah B.
dc.contributor.authorKaplancikli, Zafer A.
dc.date.accessioned2020-07-09T20:58:42Z
dc.date.available2020-07-09T20:58:42Z
dc.date.issued2020
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.urihttps://doi.org/10.1002/ardp.202000008
dc.identifier.urihttps://hdl.handle.net/11421/23980
dc.descriptionKaraduman, Abdullah Burak/0000-0002-0434-1334en_US
dc.descriptionWOS: 000519092100001en_US
dc.descriptionPubMed: 32159244en_US
dc.description.abstractAromatase is involved in the biosynthesis of estrogen and thus is a critical target for breast cancer. in this study, to identify new aromatase enzyme inhibitors, seven 3-[4-(5-methyl-1H-benzo[d]imidazol-2-yl)phenyl]-6-(substituted phenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives were synthesized. First, a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was performed to determine the inhibitory activity of the synthesized compounds on the MCF-7 cell line. the aromatase inhibitory activity was determined for the active compounds 5b, 5c, 5e, and 5g on the MCF-7 cell line. Compound 5g showed significant aromatase inhibitory activity (IC50 = 0.037 +/- 0.001 mu M). Interestingly, this compound, which bears a difluoro substituent at positions 2 and 4 of the phenyl ring, displayed the most potent aromatase inhibitory activity without significant cytotoxicity to a normal healthy cell line (NIH3T3). Furthermore, the interactions between the best active compounds and the active site of the enzyme were analyzed through a docking study. the results of this study determined that benzimidazole-triazolothiadiazine derivatives are promising compounds that should be further developed as a novel class of aromatase inhibitors.en_US
dc.language.isoengen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.isversionof10.1002/ardp.202000008en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectaromataseen_US
dc.subjectbenzimidazoleen_US
dc.subjectMCF-7en_US
dc.subjectmolecular dockingen_US
dc.subjecttriazolothiadiazineen_US
dc.titleSynthesis and docking study of benzimidazole-triazolothiadiazine hybrids as aromatase inhibitorsen_US
dc.typearticleen_US
dc.relation.journalArchiv Der Pharmazieen_US
dc.contributor.departmentAnadolu Üniversitesien_US
dc.identifier.volume353en_US
dc.identifier.issue5en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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