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

• Published in: Current medicinal chemistry Vol. 28; no. 33; p. 6805
• Main Authors: Kumar, Vishal, Dhawan, Sanjeev, Girase, Pankaj Sanjay, Awolade, Paul, Shinde, Suraj Raosaheb, Karpoormath, Rajshekhar, Singh, Parvesh
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 25.10.2021
• Subjects: Antineoplastic Agents - pharmacology; Chalcones - pharmacology; Humans; Neoplasms - drug therapy; Structure-Activity Relationship; anticancer hybrids; mechanism of action; cancer; structure-activity relationship; Chalcone; molecular target
• ISSN: 1875-533X
• DOI: 10.2174/0929867328666210322102836

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.