2009
DOI: 10.1021/jm801590u
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Chalcones: A Valid Scaffold for Monoamine Oxidases Inhibitors

Abstract: A large series of substituted chalcones have been synthesized and tested in vitro for their ability to inhibit human monoamine oxidases A and B (hMAO-A and hMAO-B). While all the compounds showed hMAO-B selective activity in the micro- and nanomolar ranges, the best results were obtained in the presence of chlorine and hydroxyl or methoxyl substituents. To better understand the enzyme-inhibitor interaction and to explain the selectivity of the most active compounds toward hMAO-B, molecular modeling studies wer… Show more

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Cited by 174 publications
(121 citation statements)
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“…1). [14][15][16][17][18][19][20] Chalcones are intermediates in the biosynthesis of flavonoids and are reported to possess a wide range of biological activities. 21,22 Since chalcones are relatively facile to prepare in the laboratory, they often serve as reagents and intermediates in organic chemistry.…”
mentioning
confidence: 99%
“…1). [14][15][16][17][18][19][20] Chalcones are intermediates in the biosynthesis of flavonoids and are reported to possess a wide range of biological activities. 21,22 Since chalcones are relatively facile to prepare in the laboratory, they often serve as reagents and intermediates in organic chemistry.…”
mentioning
confidence: 99%
“…Moreover, QSAR and in vitro study performed by Chimenti et al revealed that chalcones are valid scaffolds for the inhibition of MAO. 23 In this study, some of the chalcones showed a very high selectivity index when compared to the standard antidepressants clorgyline, deprenyl, iproniazid, and moclobemide. Based on this perception, we decided to synthesize derivatives of oxindoles in the form of chalcones.…”
Section: Introductionmentioning
confidence: 65%
“…It was observed that licochalcone A suppressed the growth of all the three tested bladder cancer cell lines in a dose-dependent manner (Figure 1). ERK 1/2 has been reported to be involved in drug resistance [11][12][13][14][15][16][17]. …”
Section: Effect Of Licochalcone a On Bladder Cancer Cell Growth And Ementioning
confidence: 99%
“…Licochalcone A (LA), an oxygenated chalcone was isolated from the roots of the Chinese liquorice (Glycyrrhiza uralensis). It is reported to exhibit various bioactive properties including antiparasitic, estrogenic, antimalarial and antitumor activities [14]. LA regulates cell growth and induces cell apoptosis in prostate cancer cell lines [15].…”
Section: Introductionmentioning
confidence: 99%