There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for
cancer prevention and
therapy.
Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices,
tea, beer, fruits and vegetables, consist of open-chain
flavonoids in which the two aromatic rings are joined by a three-
carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with
cysteine residues in
proteins, some lead
chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in
cancers. These pathways and targets that are affected by
chalcones include MDM2/p53,
tubulin,
proteasome,
NF-kappa B, TRIAL/
death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3,
AP-1, NRF2, AR, ER,
PPAR-γ and β-
catenin/Wnt. Compared to current
cancer targeted therapeutic drugs,
chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of
chalcones from substituted
benzaldehydes and
acetophenones also makes them an attractive
drug scaffold. Therefore, this review is focused on molecular targets of
chalcones and their potential implications in
cancer prevention and
therapy.