Abstract
Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.
Highlights
Cancer is caused by the uncontrolled growth of cells and is a multifactorial disease that claims millions of lives each year worldwide
We summarize the effects of structure–activity relationship (SAR) substitution patterns on chalcone anticancer properties including electron-donating (-OH and -OCH3 ), electron-withdrawing (-Cl, -Br, and -F) and chalcone–metal complexes (Figure 5)
Further mechanistic studies demonstrated that TChal could bind and degrade chromosome region maintenance 1 (CRM1), a nuclear export receptor involved in the active transport of tumor suppressors, and increase heat-shock protein 40 (HSP40) expression in U2OS osteosarcoma cells; the interaction of HSP40 with mouse double minute 2 (MDM2) blocked MDM2-mediated ubiquitination of p53, leading to the enhanced stability and activation of p53 [128,130]
Summary
Cancer is caused by the uncontrolled growth of cells and is a multifactorial disease that claims millions of lives each year worldwide. Chalcone family members have received considerable attention because of the possibilities for their synthetic and biosynthetic production and because of the scope of their biological activities, including anticancer [10], anti-inflammatory [11], antidiabetic [12], cancer chemopreventive [13], antioxidant [14], antimicrobial [15], antileishmanial [16] and antimalarial activities [17]. Hybridization of the chalcone with other pharmacophores anticancer pharmacophores hybrids that have that the potential to overcome drug resistance and improve therapeutic produces hybrids have the potential to overcome drug resistance and improve therspecificity, rendering rendering it a promising for developing novel anticancer agents.
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