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|Title:||Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors|
Chulabhorn Research Institute
Ministry of Education
|Keywords:||Biochemistry, Genetics and Molecular Biology;Chemistry|
|Citation:||Bioorganic Chemistry. Vol.93, (2019)|
|Abstract:||© 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.|
|Appears in Collections:||Scopus 2019|
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