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https://ir.swu.ac.th/jspui/handle/123456789/12238
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DC Field | Value | Language |
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dc.contributor.author | Chamduang C. | - |
dc.contributor.author | Pingaew R. | - |
dc.contributor.author | Prachayasittikul V. | - |
dc.contributor.author | Prachayasittikul S. | - |
dc.contributor.author | Ruchirawat S. | - |
dc.contributor.author | Prachayasittikul V. | - |
dc.date.accessioned | 2021-04-05T03:02:22Z | - |
dc.date.available | 2021-04-05T03:02:22Z | - |
dc.date.issued | 2019 | - |
dc.identifier.issn | 452068 | - |
dc.identifier.other | 2-s2.0-85073107177 | - |
dc.identifier.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85073107177&doi=10.1016%2fj.bioorg.2019.103327&partnerID=40&md5=d993e1f6df5ce14efacb18134bcece56 | - |
dc.identifier.uri | https://ir.swu.ac.th/jspui/handle/123456789/12238 | - |
dc.description.abstract | Novel 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.subject | Tetrahydroisoquinoline | - |
dc.subject | Aromatase inhibitor | - |
dc.subject | Tetrahydroisoquinoline | - |
dc.subject | Triazole | - |
dc.subject | Unclassified drug | - |
dc.subject | Aromatase inhibitor | - |
dc.subject | Tetrahydroisoquinoline derivative | - |
dc.subject | Triazole derivative | - |
dc.subject | Alkylation | - |
dc.subject | Article | - |
dc.subject | Cytotoxicity | - |
dc.subject | Drug synthesis | - |
dc.subject | Enzyme active site | - |
dc.subject | Human | - |
dc.subject | Hydrogen bond | - |
dc.subject | IC50 | - |
dc.subject | Molecular docking | - |
dc.subject | Priority journal | - |
dc.subject | Structure activity relation | - |
dc.subject | Chemistry | - |
dc.subject | Drug screening | - |
dc.subject | Procedures | - |
dc.subject | Spectroscopy | - |
dc.subject | Synthesis | - |
dc.subject | Tumor cell line | - |
dc.subject | Aromatase Inhibitors | - |
dc.subject | Cell Line, Tumor | - |
dc.subject | Drug Screening Assays, Antitumor | - |
dc.subject | Humans | - |
dc.subject | Hydrogen Bonding | - |
dc.subject | Inhibitory Concentration 50 | - |
dc.subject | Molecular Docking Simulation | - |
dc.subject | Spectrum Analysis | - |
dc.subject | Structure-Activity Relationship | - |
dc.subject | Tetrahydroisoquinolines | - |
dc.subject | Triazoles | - |
dc.title | Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors | - |
dc.type | Article | - |
dc.rights.holder | Scopus | - |
dc.identifier.bibliograpycitation | Bioorganic Chemistry. Vol 93, (2019) | - |
dc.identifier.doi | 10.1016/j.bioorg.2019.103327 | - |
Appears in Collections: | Scopus 1983-2021 |
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