title: (Iso)flav(an)ones, chalcones, catechins, and theaflavins as anticarcinogens: mechanisms, anti-multidrug resistance and QSAR studies.
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.
authors: Instituto de Biología y Medicina Molecular IBIMOL (ex PRALIB) (UBA-CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina. andrewgmercader@gmail.com
authors: Andrew G
authors: AG
authors: Mercader
authors: Alicia B
authors: AB
authors: Pomilio
mesh_terms: D000818:Animals; D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D044946:Biflavonoids / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002392:Catechin / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007529:Isoflavones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D009369:Neoplasms / Q000378:metabolism / Q000517:prevention & control*; D021281:Quantitative Structure-Activity Relationship
chemical_list: D016588:Anticarcinogenic Agents; D044946:Biflavonoids; D047188:Chalcones; D007529:Isoflavones; C056068:theaflavin; D002392:Catechin