title: Chalcones as Promising Lead Compounds on Cancer Therapy.
abstract: Chalcones constitute a group of phenolic compounds that command an increasing interest on cancer research. Natural chalcones are widespread through the plant kingdom. The most abundant and investigated chalcones are isoliquiritigenin, flavokawain and xanthohumol, which are present in the Fabaceae, Piperaceae, Cannabaceae, and Moraceae families. These chalcones have been shown to be promising lead antitumor-chemopreventive drugs by three different activities: antioxidants, cytotoxic and apoptosis inducers. In the recent years, SAR (structure-activity relationship) has contributed towards the improvement of anticancer properties of chalcones by substituting aryl rings and introducing heterocyclic moieties. This review summarizes the anticancer activities shown by natural chalcones and the SAR and describes how different chemical moiety modifications could lead them to be therapeutically useful in the treatment of cancer.
authors.forename: Antonio J
authors.initials: AJ
authors.lastname: León-González
authors.forename: Nuria
authors.initials: N
authors.lastname: Acero
authors.forename: Dolores
authors.initials: D
authors.lastname: Muñoz-Mingarro
authors.forename: Inmaculada
authors.initials: I
authors.lastname: Navarro
authors.affiliation: Departamento de Farmacologia, Facultad de Farmacia, Universidad de Sevilla, Prof. Garcia Gonzalez 2, 41012 Sevilla (Spain). carmenmc@us.es.
authors.forename: Carmen
authors.initials: C
authors.lastname: Martín-Cordero
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002599:Chalcone / Q000737:chemistry / Q000627:therapeutic use*; D016503:Drug Delivery Systems; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D017346:Protein Serine-Threonine Kinases / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects; D000097782:NF-kappaB-Inducing Kinase
chemical_list: D000970:Antineoplastic Agents; D002599:Chalcone; D017346:Protein Serine-Threonine Kinases; D000097782:NF-kappaB-Inducing Kinase