Title:Recent Advances in Chalcone-Based Anticancer Heterocycles: A Structural and Molecular Target Perspective
Volume: 28
Issue: 33
Author(s): Vishal Kumar, Sanjeev Dhawan, Pankaj Sanjay Girase, Paul Awolade, Suraj Raosaheb Shinde, Rajshekhar Karpoormath*Parvesh Singh*
Affiliation:
- Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Durban-4000,South Africa
- School of Chemistry and Physics, University of KwaZulu-Natal (Westville Campus), Private Bag X01, Scottsville, Durban,South Africa
Keywords:
Chalcone, anticancer hybrids, cancer, molecular target, mechanism of action, structure-activity relationship.
Abstract: Chalcones are an interesting class of compounds endowed with a plethora of
biological activities beneficial to human health. These chemotypes have continued to attract
increased research attention over the years; hence, numerous natural and synthetic
chalcones have found with interesting anticancer activities through the inhibition of various
molecular targets including ABCG2, BCRP, P-glycoprotein, 5α-reductase, Androgen
Receptor (AR), Histone Deacetylases (HDAC), Sirtuin 1, proteasome, Vascular Endothelial
Growth Factor (VEGF), Cathepsin-K, tubulin, CDC25B phosphatase, Topoisomerase,
EBV, NF-κB, mTOR, BRAF, and Wnt/β-catenin. Moreover, the study of intrinsic mechanisms
of action, particularly relating to specific cellular pathways and modes of engagement
with molecular targets, may help medicinal chemists to develop more effective, selective,
and cost-effective chalcone-based anticancer drugs. This review, therefore, sheds
light on the effect of structural variations on the anticancer potency of chalcone hybrids
reported in 2018-2019 alongside their mechanism of action, molecular targets, and potential
impacts on effective cancer chemotherapy.