Abstract
Naphthoflavones are synthetic flavonoids containing a conjugated phenyl group attached to A-ring of flavones. Most of their synthetic studies involved the Baker–Venkataraman rearrangement and subsequent cyclization catalyzed by acid. Based on their special structural features, these synthetic flavones exert pronounced influences on the metabolism of various endogenous and exogenous substances as well as the bioactivation of certain procarcinogens. Several mechanisms of these effects have been established, including the potent inhibition on CYP1 and aromatase, allosteric activation of CYP3A4 and/or activation of AhR. Furthermore, they have also been identified as CFTR activators, BCRP inhibitors and/or anticancer agents. All of the findings suggest that these synthetic ones are a series of promising lead compounds in cystic fibrosis therapeutic and anticancer drug discovery. This review primarily focuses on the structure, chemistry and pharmacology of naphthoflavones, while benzothioflavones, benzoflavanones, benzoflavans and benzochalcones as their analogues are also included.
Keywords: Anticancer, cystic fibrosis therapy, flavonoids, naphthoflavones, pharmacology, SARs.
Mini-Reviews in Medicinal Chemistry
Title:Structure, Chemistry and Pharmacology of Naphthoflavones
Volume: 13 Issue: 9
Author(s): Jiahua Cui and Shaoshun Li
Affiliation:
Keywords: Anticancer, cystic fibrosis therapy, flavonoids, naphthoflavones, pharmacology, SARs.
Abstract: Naphthoflavones are synthetic flavonoids containing a conjugated phenyl group attached to A-ring of flavones. Most of their synthetic studies involved the Baker–Venkataraman rearrangement and subsequent cyclization catalyzed by acid. Based on their special structural features, these synthetic flavones exert pronounced influences on the metabolism of various endogenous and exogenous substances as well as the bioactivation of certain procarcinogens. Several mechanisms of these effects have been established, including the potent inhibition on CYP1 and aromatase, allosteric activation of CYP3A4 and/or activation of AhR. Furthermore, they have also been identified as CFTR activators, BCRP inhibitors and/or anticancer agents. All of the findings suggest that these synthetic ones are a series of promising lead compounds in cystic fibrosis therapeutic and anticancer drug discovery. This review primarily focuses on the structure, chemistry and pharmacology of naphthoflavones, while benzothioflavones, benzoflavanones, benzoflavans and benzochalcones as their analogues are also included.
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Cite this article as:
Cui Jiahua and Li Shaoshun, Structure, Chemistry and Pharmacology of Naphthoflavones, Mini-Reviews in Medicinal Chemistry 2013; 13 (9) . https://dx.doi.org/10.2174/1389557511313090010
DOI https://dx.doi.org/10.2174/1389557511313090010 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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