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Current Medicinal Chemistry

Eiditor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

(Iso)Flav(an)ones, Chalcones, Catechins, and Theaflavins as Anticarcinogens: Mechanisms, Anti-Multidrug Resistance and QSAR Studies

Author(s): Andrew G. Mercader and Alicia B. Pomilio

Volume 19 , Issue 25 , 2012

Page: [4324 - 4347] Pages: 24

DOI: 10.2174/092986712802884277

Price: $58

Abstract

Flavonoids have shown anticarcinogenic activity in cancer cell lines, animal models, and some human studies. Quantitative structure-activity relationship (QSAR) models have become useful tools for identification of promising lead compounds in anticancer drug development. However, epidemiological and clinical studies are still scarce. Compounds with flavonoid scaffold have been the subject of many mechanistic studies in cells, but information on human chemopreventive properties is still missing. The knowledge of the mechanisms of action, anti-multidrug resistance, and QSAR studies on flavonoids and related compounds may help to enhance research on these compounds and their bioactivity. Therefore, once the issue is introduced, the mechanisms involved, and QSAR studies developed to predict the activity and toxicity of these chemicals to biological systems are discussed. QSAR studies on flavonoids as inhibitors of breast cancer resistance protein (BCRP/ABCG2), 17β-hydroxysteroid dehydrogenase (17β-HSD), PIM-1 kinase and cyclin-dependent kinases (CDKs) are analyzed. Combined treatment of flavonoids with TRAIL and current chemotherapy agents is also discussed as a promising cancer chemoprevention and/or therapy.

Keywords: Anticarcinogens, flavonoids, (iso)flavones, flavanones, catechins, chalcones, QSAR, theaflavins, TRAIL, flavonoids/TRAIL, flavonoids/chemotherapy


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