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https://ir.swu.ac.th/jspui/handle/123456789/12238
ชื่อเรื่อง: | Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors |
ผู้แต่ง: | Chamduang C. Pingaew R. Prachayasittikul V. Prachayasittikul S. Ruchirawat S. Prachayasittikul V. |
Keywords: | Tetrahydroisoquinoline Aromatase inhibitor Tetrahydroisoquinoline Triazole Unclassified drug Aromatase inhibitor Tetrahydroisoquinoline derivative Triazole derivative Alkylation Article Cytotoxicity Drug synthesis Enzyme active site Human Hydrogen bond IC50 Molecular docking Priority journal Structure activity relation Chemistry Drug screening Procedures Spectroscopy Synthesis Tumor cell line Aromatase Inhibitors Cell Line, Tumor Drug Screening Assays, Antitumor Humans Hydrogen Bonding Inhibitory Concentration 50 Molecular Docking Simulation Spectrum Analysis Structure-Activity Relationship Tetrahydroisoquinolines Triazoles |
วันที่เผยแพร่: | 2019 |
บทคัดย่อ: | 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. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85073107177&doi=10.1016%2fj.bioorg.2019.103327&partnerID=40&md5=d993e1f6df5ce14efacb18134bcece56 https://ir.swu.ac.th/jspui/handle/123456789/12238 |
ISSN: | 452068 |
Appears in Collections: | Scopus 1983-2021 |
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