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 |
|