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Aromatase inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies.

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dc.contributor.authorOZCAN-SEZER, S
dc.contributor.authorINCE, E
dc.contributor.authorAkdemir, ATİLLA
dc.contributor.authorCEYLAN, ÖÖ
dc.contributor.authorSuzen, S
dc.contributor.authorGURER-ORHAN, H
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T12:41:53Z
dc.date.available2019-10-05T12:41:53Z
dc.date.issued2019-05-01
dc.description.abstractA causal association is reported between prolonged exposures to elevated levels of estrogen and breast cancer. Therefore inhibiting aromatase (CYP19A), which catalyses the conversion of androgens to estrogens, is an important approach in prevention and treatment of estrogen receptor positive (ER+) breast cancer. Melatonin, a natural indolic hormone, is reported to prevent free radical induced carcinogenesis and block local estrogen synthesis in breast tissue via aromatase inhibition. However several features of melatonin limit its therapeutic use. In the present study aromatase inhibiting potential of 2-methyl indole hydrazones are investigated, and compared with melatonin, by two in vitro models; a cell-free assay using a fluorescence substrate and a cell-based assay where cell proliferation was determined in ER + human breast cancer cells (MCF-7 BUS) in the absence of estrogen and the presence of testosterone. Aromatase inhibitory effect is also explored by molecular modelling studies. In biological activity assays monochloro substituted indole hydrazones were found to have stronger aromatase inhibitory activity among all tested derivatives and were more active than melatonin. This finding is further confirmed by molecular modelling. These results may be useful in the design and synthesis of novel melatonin analogues with higher inhibitory potency against aromatase.en
dc.description.sponsorshipTürkiye Bilimsel Ve Teknolojik Araştırma Kurumu ( Tübitak )
dc.identifier10.1016/j.foodchem.2012.10.056
dc.identifier.citationOZCAN-SEZER S., INCE E., Akdemir A., CEYLAN Ö., Suzen S., GURER-ORHAN H., -Aromatase inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies.-, Xenobiotica; the fate of foreign compounds in biological systems, cilt.49, ss.549-556, 2019
dc.identifier.doi10.1080/00498254.2018.1482029
dc.identifier.pubmed29804490
dc.identifier.scopus85053433543
dc.identifier.trdizintrdizin
dc.identifier.urihttps://hdl.handle.net/20.500.12645/331
dc.identifier.urihttps://doi.org/10.1080/00498254.2018.1482029
dc.identifier.wosWOS:000461389600006
dc.language.isoen
dc.subjectAromatase inhibition
dc.subjectmelatonin analogues
dc.subjectmolecular modelling
dc.subjectBreast cancer
dc.subjectAromatase inhibition
dc.titleAromatase inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies.
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameFOOD CHEMISTRY
local.avesis.id04aaf74b-9b71-4f46-987f-4a033956bfee
local.avesis.response201
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
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