Publication: Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors
Issued Date
2019-12-01
Resource Type
ISSN
10902120
00452068
00452068
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2-s2.0-85073107177
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Mahidol University
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SCOPUS
Bibliographic Citation
Bioorganic Chemistry. Vol.93, (2019)
Suggested Citation
Chanamon Chamduang, Ratchanok Pingaew, Veda Prachayasittikul, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors. Bioorganic Chemistry. Vol.93, (2019). doi:10.1016/j.bioorg.2019.103327 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/50014
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Title
Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors
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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.