Chanamon ChamduangRatchanok PingaewVeda PrachayasittikulSupaluk PrachayasittikulSomsak RuchirawatVirapong PrachayasittikulChulabhorn Research InstituteMahidol UniversitySrinakharinwirot UniversityMinistry of Education2020-01-272020-01-272019-12-01Bioorganic Chemistry. Vol.93, (2019)10902120004520682-s2.0-85073107177https://repository.li.mahidol.ac.th/handle/20.500.14594/50014© 2019 Elsevier Inc. 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.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryArticleSCOPUS10.1016/j.bioorg.2019.103327