{"title":"7-羟基黄酮作为雌酮和雌二醇生物合成抑制剂的评价","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":"{\"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}","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}
Evaluation of 7-Hydroxy-Flavones as Inhibitors of Oestrone and Oestradiol Biosynthesis
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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