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.
Keywords: Apoptosis, cancer, chalcone, chemoprevention, flavonoid, synthesis, tubulin.
Current Medicinal Chemistry
Title:Chalcones as Promising Lead Compounds on Cancer Therapy
Volume: 22 Issue: 30
Author(s): Antonio J. Leon-Gonzalez, Nuria Acero, Dolores Munoz-Mingarro, Inmaculada Navarro and Carmen Martin-Cordero
Affiliation:
Keywords: Apoptosis, cancer, chalcone, chemoprevention, flavonoid, synthesis, tubulin.
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.
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Cite this article as:
Leon-Gonzalez J. Antonio, Acero Nuria, Munoz-Mingarro Dolores, Navarro Inmaculada and Martin-Cordero Carmen, Chalcones as Promising Lead Compounds on Cancer Therapy, Current Medicinal Chemistry 2015; 22 (30) . https://dx.doi.org/10.2174/0929867322666150729114829
DOI https://dx.doi.org/10.2174/0929867322666150729114829 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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