Chalcone Scaffolds as Anticancer Drugs: A Review on Molecular Insight in Action of Mechanisms and Anticancer Properties

Cancer is the deadliest disease worldwide and the development of safer chemical entities to treat cancer is one of the major challenges of medicinal chemistry. The emergence of new cases every year and the development of multiple drug resistance against available molecular entities have turned the focus of researchers towards natural products. Chalcones are pharmacologically active compounds, present in plants, which have been derivatized and screened by many researchers for the treatment of cancer. Chalcones, consist of 1,3-diaryl-2propen-1-one, is one such class exhibiting broad anticancer activities against various cancerous cell lines. The objective of this review article is to analyze the antitumor activity of the reported chalcones via distinct mechanisms adopted by these molecules underlying their inhibitory activity. The primary focus of this review is to bring the attention of researchers towards the latest and important chalcones and their derivatives having potent anticancer activity adding their possible action of mechanisms against cancerous cell lines The recent literature was surveyed and it was found that chalcone analogs with electron donating groups, indolyl, quinolone, pyrazol-ol, hydroxyaminobenzamide, hydroxamic acid and pyridyl-indole groups have shown promise as potential anticancer agents following various mechanisms. Most chalcones were found to induce significant cell cycle arrest at G2/M phase hence leading to apoptosis. A number of synthetic chalcones exhibited higher efficacy due to their ability of potent tubulin polymerization as well as dynamic enzyme inhibitory activity. This review is an immense compilation of research regarding the mechanism of action of chalcones and their identification as a promising anticancer agent for future drug developments. Thus, this review article would pave the way and provide ample opportunities to design future generations of novel, highly efficacious anticancer molecules with minimal toxicity.

Automated summary

This review discusses the anticancer activity of chalcones and their potential mechanisms of action. Research has shown that chalcone analogs with specific functional groups have promising anticancer properties following various pathways.