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Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors

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dc.contributor.authorChamduang C.
dc.contributor.authorPingaew R.
dc.contributor.authorPrachayasittikul V.
dc.contributor.authorPrachayasittikul S.
dc.contributor.authorRuchirawat S.
dc.contributor.authorPrachayasittikul V.
dc.date.accessioned2021-04-05T03:02:22Z
dc.date.available2021-04-05T03:02:22Z
dc.date.issued2019
dc.date.issuedBE2562
dc.description.abstractNovel thirteen triazole-tetrahydroisoquinoline derivatives (2a-m) were synthesized and evaluated for their aromatase inhibitory activities. Seven triazoles showed significant aromatase inhibitory activity (IC50 = 0.07–1.9 μM). Interestingly, the analog bearing naphthalenyloxymethyl substituent at position 4 of the triazole ring (2i) displayed the most potent aromatase inhibitory activity (IC50 = 70 nM) without significant cytotoxicity to a normal cell. Molecular docking also suggested that the direct H-bonding interaction with residue Thr310 may be responsible for a striking inhibitory effect of the most potent compound 2i. © 2019 Elsevier Inc.
dc.format.mimetypeapplication/pdf
dc.identifier.citationBioorganic Chemistry. Vol 93, (2019)
dc.identifier.doi10.1016/j.bioorg.2019.103327
dc.identifier.issn452068
dc.identifier.other2-s2.0-85073107177
dc.identifier.urihttps://hdl.handle.net/20.500.14740/5061
dc.rights.holderScopus
dc.subject.otherTetrahydroisoquinoline
dc.subject.otherAromatase inhibitor
dc.subject.otherTetrahydroisoquinoline
dc.subject.otherTriazole
dc.subject.otherUnclassified drug
dc.subject.otherAromatase inhibitor
dc.subject.otherTetrahydroisoquinoline derivative
dc.subject.otherTriazole derivative
dc.subject.otherAlkylation
dc.subject.otherArticle
dc.subject.otherCytotoxicity
dc.subject.otherDrug synthesis
dc.subject.otherEnzyme active site
dc.subject.otherHuman
dc.subject.otherHydrogen bond
dc.subject.otherIC50
dc.subject.otherMolecular docking
dc.subject.otherPriority journal
dc.subject.otherStructure activity relation
dc.subject.otherChemistry
dc.subject.otherDrug screening
dc.subject.otherProcedures
dc.subject.otherSpectroscopy
dc.subject.otherSynthesis
dc.subject.otherTumor cell line
dc.subject.otherAromatase Inhibitors
dc.subject.otherCell Line, Tumor
dc.subject.otherDrug Screening Assays, Antitumor
dc.subject.otherHumans
dc.subject.otherHydrogen Bonding
dc.subject.otherInhibitory Concentration 50
dc.subject.otherMolecular Docking Simulation
dc.subject.otherSpectrum Analysis
dc.subject.otherStructure-Activity Relationship
dc.subject.otherTetrahydroisoquinolines
dc.subject.otherTriazoles
dc.titleNovel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors
dc.typeArticle
dspace.entity.typePublication
swu.datasource.scopushttps://www.scopus.com/inward/record.uri?eid=2-s2.0-85073107177&doi=10.1016%2fj.bioorg.2019.103327&partnerID=40&md5=d993e1f6df5ce14efacb18134bcece56

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