Title:Molecular Targeted Approaches to Cancer Therapy and Prevention Using Chalcones
Volume: 14
Issue: 2
Author(s): Danielle D. Jandial, Christopher A. Blair, Saiyang Zhang, Lauren S. Krill, Yan-Bing Zhang and Xiaolin Zi
Affiliation:
Keywords:
Chalcones, molecular targets, bioactive dietary compounds, chemoprevention.
Abstract: 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.
