Chromenylchalcones with inhibitory effects on monoamine oxidase B

Title
Chromenylchalcones with inhibitory effects on monoamine oxidase B
Authors
조근형안승현김봉규박혜리김영화추현아고동수정유훈안중훈임융호
Keywords
MOA-B; monoamine oxidase; Chromenylchalcone; molecular modeling; SAR; Flavonoid; In silico docking; Monoamine oxidase B
Issue Date
2013-12
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 21, NO 24, 7890-7897
Abstract
Structure–activity relationship (SAR) calculations were used to find monoamine oxidase-B (MAO-B) inhibitors by identifying pharmacophores exhibiting high inhibitory activities. Several such chromenylchalcones were designed and synthesized accordingly. Their inhibitory effects on MAO-B were determined using an HPLC-based method and an MAO-B enzyme assay kit. (E)-3-(6-Methoxy-2H-chromen-3-yl)-1-(2-methoxyphenyl)prop-2-en-1-one exhibited a half-maximal inhibitory concentration of 320 nM. Its molecular-level binding mode with the three-dimensional structure of MAO-B was elucidated using an in silico docking study. The chromenylchalcone scaffold, which is derived from natural products including isoflavonoids and chalcones, had not been previously reported as an MAO-B inhibitor
URI
http://pubs.kist.re.kr/handle/201004/46827
ISSN
09680896
Appears in Collections:
KIST Publication > Article
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