Recent Advances in Chalcone-Based Anticancer Heterocycles: A Structural and Molecular Target Perspective

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.

Cite this article as:

Kumar Vishal , Dhawan Sanjeev , Girase Sanjay Pankaj , Awolade Paul , Shinde Raosaheb Suraj , Karpoormath Rajshekhar *, Singh Parvesh *, Recent Advances in Chalcone-Based Anticancer Heterocycles: A Structural and Molecular Target Perspective, Current Medicinal Chemistry 2021; 28 (33) . https://dx.doi.org/10.2174/0929867328666210322102836