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Title: Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors
Authors: Chanamon Chamduang
Ratchanok Pingaew
Veda Prachayasittikul
Supaluk Prachayasittikul
Somsak Ruchirawat
Virapong Prachayasittikul
Chulabhorn Research Institute
Mahidol University
Srinakharinwirot University
Ministry of Education
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry
Issue Date: 1-Dec-2019
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.
ISSN: 10902120
Appears in Collections:Scopus 2019

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