{"title":"Evaluation of 7-Hydroxy-Flavones as Inhibitors of Oestrone and Oestradiol Biosynthesis","authors":"T. K. Vinh, P. Nicholls, A. Kirby, C. Simons","doi":"10.1080/14756360109162390","DOIUrl":null,"url":null,"abstract":"A series of 4-aryl substituted 7-hydroxy-flavones were prepared using the three-step Baker-Venka-taraman synthesis in good overall yields. The flavones were all evaluated in vitro for inhibitory activity against aromatase (P450AROM/ CYP19), using human placental microsomes, and for inhibitory activity against 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD-1) using human placental cytosol. The phenyl, 4-fluoro-phenyl and 4-bromo-phenyl derivatives displayed moderate inhibitory activity against P450AROM (IC50 17.2, 13.5 and 10.1 μM, respectively), none of the flavones, including the standard genistein, displayed any inhibitory activity against 17β-HSD type 1 at 100 μM concentration.","PeriodicalId":15776,"journal":{"name":"Journal of enzyme inhibition","volume":"4 1","pages":"417 - 424"},"PeriodicalIF":0.0000,"publicationDate":"2001-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"4","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of enzyme inhibition","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/14756360109162390","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 4
Abstract
A series of 4-aryl substituted 7-hydroxy-flavones were prepared using the three-step Baker-Venka-taraman synthesis in good overall yields. The flavones were all evaluated in vitro for inhibitory activity against aromatase (P450AROM/ CYP19), using human placental microsomes, and for inhibitory activity against 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD-1) using human placental cytosol. The phenyl, 4-fluoro-phenyl and 4-bromo-phenyl derivatives displayed moderate inhibitory activity against P450AROM (IC50 17.2, 13.5 and 10.1 μM, respectively), none of the flavones, including the standard genistein, displayed any inhibitory activity against 17β-HSD type 1 at 100 μM concentration.
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