Abstract
Cancer is a condition caused by many mechanisms (genetic, immune, oxidation, and inflammatory). Anticancer therapy aims to destroy or stop the growth of cancer cells. Resistance to treatment is theleading cause of the inefficiency of current standard therapies. Targeted therapies are the most effective due to the low number of side effects and low resistance. Among the small molecule natural compounds, flavonoids are of particular interest for theidentification of new anticancer agents. Chalcones are precursors to all flavonoids and have many biological activities. The anticancer activity of chalcones is due to the ability of these compounds to act on many targets. Natural chalcones, such as licochalcones, xanthohumol (XN), panduretin (PA), and loncocarpine, have been extensively studied and modulated. Modification of the basic structure of chalcones in order to obtain compounds with superior cytotoxic properties has been performed by modulating the aromatic residues, replacing aromatic residues with heterocycles, and obtaining hybrid molecules. A huge number of chalcone derivatives with residues such as diaryl ether, sulfonamide, and amine have been obtained, their presence being favorable for anticancer activity. Modification of the amino group in the structure of aminochalconesis always favorable for antitumor activity. This is why hybrid molecules of chalcones with different nitrogen hetercycles in the molecule have been obtained. From these, azoles (imidazole, oxazoles, tetrazoles, thiazoles, 1,2,3-triazoles, and 1,2,4-triazoles) are of particular importance for the identification of new anticancer agents.
Highlights
Cancer is a significant public health problem that has a small number of effective therapies, a poor prognosis, and a high mortality rate [1]
These results suggest that LA-induced apoptosis is associated with poly (ADP-ribose) polymerase (PARP)/Bcl-2 pathway [177]
Literature indicates that a concentration of 9 μg/mL of PA completely inhibits the growth of MCF-7 cells and HT-29 cells [205].The chalcone has anticancer properties on various cell types, including melanoma, colon adenocarcinoma, and prostate cancer [204].Liu el al. highlighted the cytotoxic effect of the chalcone on MCF-7, T47D, and MCF-10A
Summary
Cancer is a significant public health problem that has a small number of effective therapies, a poor prognosis, and a high mortality rate [1]. Natural small molecule compounds in class of flavonoids are considered to have remarkable physiological effects, have non-mutagenic properties in the human body, and have attracted increasing interest for the identification of new anticancer agents. Chalcones, under certain conditions, have oxidizing properties This effect may be associated with antitumor activity of these compounds and is based on mechanisms such as increased superoxide formation, cellular glutathione depletion, and phenoxide radical generation. Available studies have demonstrated targeted activity of chalcones on numerous kinases, microtubules, polytherapy-resistant proteins, and various signaling pathways associated with cell survival and death [138] Interesting structure of these compounds and various biological activities have led to approval of new drugs from chalcone class, such as metochalcone (an anticoleretic drug) and sofalcone (an antiulcer drug) (Figure 5) [139,140]. The purpose of this article is to summarize information obtained experimentally and in silico about anticancer activity of some natural and synthetic chalcones
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