What is it about?
Flavokawain B (FKB) is a natural chalcone extracted from the roots of Piper methysticum and has been proven to be a potential cytotoxic compound. Using the partial structure of flavokawain B, about 23 analogues have been synthesized. Among them, compounds 8, 13 and 23 were found in new FKB derivatives. All compounds were evaluated for their cytotoxic properties against two breast cancer cell lines, MCF-7 and MDA-MB-231, thus establishing the structure-activity relationship.
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Why is it important?
Twenty-three FKB derivatives were synthesized by Claisen–Schmidt condensation reaction. Three FKB derivatives were found to be new chalcones. The chalcones with electron-withdrawing and electron-donating substituents had effects on cytotoxicity. The FKB derivatives with electron-withdrawing groups in ring B exhibited potential cytotoxic effects on breast cancer cell lines, while the presence of the substituted electron-donating groups showed lower cytotoxic effects on MCF-7 and MDA-MB-231 cell lines. The structure-activity relationship showed FKB chalcones with different substituents and effects on cytotoxicity. The FKB skeleton is unique for anticancer agents, additionally, the presence of halogens (Cl and F) in position two and three also improve the cytotoxicity of FKB. These findings could help to improve or find new drugs for future anti-cancer agents.
Perspectives
Breast cancer is a complex disease, composed of several subtype receptors both at the molecular and clinical level, and it is still the leading causes of death globally in women. Chalcones are α,β-unsaturated carbonyl compounds with two aromatic rings (ring A and B), conjugated double bonds and a completely delocalized π-electron system. Chalcones and their related analogues display several pharmacological properties, such as anticancer, anti-inflammatory, antimalarial, antileishmanial, antimicrobial, antifungal, antioxidant and anticonvulsant activities. Chalcones have gained strong attention from scientists searching for new pharmacological active analogues.
Assoc. Prof. Dr. Syed Adnan Ali Shah
Universiti Teknologi MARA
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This page is a summary of: Design, Synthesis and Docking Studies of Flavokawain B Type Chalcones and Their Cytotoxic Effects on MCF-7 and MDA-MB-231 Cell Lines, Molecules, March 2018, MDPI AG,
DOI: 10.3390/molecules23030616.
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