Chalcone Scaffolds as Anticancer Drugs: A Review on Molecular Insight in Action of Mechanisms and Anticancer Properties
- 26 July 2021
- journal article
- review article
- Published by Bentham Science Publishers Ltd. in Anti-Cancer Agents in Medicinal Chemistry
- Vol. 21 (13), 1650-1670
- https://doi.org/10.2174/1871520620999201124212840
Abstract
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. Emergence of new cases every year and development of multiple drug resistance against available molecular entities has 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-2-propen-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 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 way and provide ample opportunities to design future generation of novel, highly efficacious anticancer molecules with minimal toxicity.Keywords
This publication has 96 references indexed in Scilit:
- Chalcone derivatives cause accumulation of colon cancer cells in the G2/M phase and induce apoptosisLife Sciences, 2016
- Novel indolyl-chalcones target stathmin to induce cancer cell deathCell Cycle, 2016
- Chalcone-Induced Apoptosis through Caspase-Dependent Intrinsic Pathways in Human Hepatocellular Carcinoma CellsInternational Journal of Molecular Sciences, 2016
- Flavokawain C Inhibits Cell Cycle and Promotes Apoptosis, Associated with Endoplasmic Reticulum Stress and Regulation of MAPKs and Akt Signaling Pathways in HCT 116 Human Colon Carcinoma CellsPLOS ONE, 2016
- Chalcone Scaffold in Anticancer Armamentarium: A Molecular InsightJournal of Toxicology, 2016
- Anti-cancer chalcones: Structural and molecular target perspectivesEuropean Journal of Medicinal Chemistry, 2015
- Chalcone derivatives as potential antifungal agents: Synthesis, and antifungal activityJournal of Advanced Pharmaceutical Technology & Research, 2015
- An Update on Antitumor Activity of Naturally Occurring ChalconesEvidence-Based Complementary and Alternative Medicine, 2013
- Notch SignalingCold Spring Harbor Perspectives in Biology, 2012
- Apoptosis: A Review of Programmed Cell DeathToxicologic Pathology, 2007