Molecular targets and anticancer activity of quinoline–chalcone hybrids: literature review

Mohamed, Mamdouh F. A.; Abuo‐Rahma, Gamal El‐Din A.

doi:10.1039/d0ra05594h

Cited by 106 publications

(68 citation statements)

References 227 publications

(112 reference statements)

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“…Oskuei et al obtained imidazolechalcones (Tables S1 and S2, compounds [104][105][106][107][108][109][110][111][112][113][114][115][116][117][118][119][120][121] to evaluate their ability to inhibit tubulin. The antiproliferative activity of the compounds was evaluated on four different cancer cell lines (A549, MCF-7, MCF-7/MX (a mitoxatroneresistant human breast cancer cell line), and HepG2).…”

Section: Imidazole Chalcone Derivativesmentioning

confidence: 99%

Anticancer Activity of Natural and Synthetic Chalcones

Constantinescu

Lungu²

2021

IJMS

103

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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.

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Section: Imidazole Chalcone Derivativesmentioning

confidence: 99%

Anticancer Activity of Natural and Synthetic Chalcones

Constantinescu

Lungu²

2021

IJMS

103

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“…2-quinolones (1-azacoumarins) play an important role in anticancer drug design since their derivatives have shown excellent anticancer activity through different mechanisms such as growth inhibition via apoptosis or inhibition of angiogenesis [ 11 , 12 , 13 , 14 ]. Additionally, the antineoplastic activity of these quinolones was attributed to intercalating binding to DNA [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives

et al. 2021

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A new series of hybrid molecules containing cinnamic acid and 2-quinolinone derivatives were designed and synthesized. Their structures were confirmed by 1H-NMR, 13C-NMR and mass analyses. All the synthesized hybrid molecules were assessed for their in vitro antiproliferative activity against more than one cancer cell lines. Compound 3-(3,5-dibromo-7,8-dihydroxy-4-methyl-2-oxoquinolin-1(2H)-ylamino)-3-phenylacrylic acid (5a) with IC50 = 1.89 μM against HCT-116 was proved to the most potent compound in this study, as compared to standard drug staurosporin. DNA flow cytometry assay of compound 5a revealed G2/M phase arrest and pre-G1 apoptosis. Annexin V-FITC showed that the percentage of early and late apoptosis was increased. The results of topoisomerase enzyme inhibition activity showed that the hybrid molecule 5a displays potent inhibitory activity compared with control.

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“…The α,β-unsaturated propanone fragment facilitates the conversion of chalcones to several classes of heterocyclic compounds 15 such as flavonoids, iso flavonoids 16 , pyrazoles 17 , 2-pyrazolines 18 , 19 , imidazoles and pyrimidines 20 . Chalcones and their derivatives have attracted substantial research attention 21 not only due to their ease of synthesis but also due to their varied and interesting biological activities such as HDAC inhibitory activity 22 , anticancer activities 23 , 24 , antihypertensive 25 , antimalarial 26 , 27 , antioxidant 28 , 29 , analgesic 30 , anti-inflammatory 31 , antibacterial 32 , antifungal 33 , 34 , antiulcer agents 35 , parasitic protease inhibitors 36 , antiviral 37 , anti-tuberculosis 38 and as insulin mimetic in 3T3-L1 adipocyte 39 .…”

Section: Introductionmentioning

confidence: 99%

Novel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design, synthesis, molecular docking studies and ADMET prediction

Ibrahim

Moustafa

Almalki

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Molecular targets and anticancer activity of quinoline–chalcone hybrids: literature review

Abstract: α,β-Unsaturated chalcone moieties and quinoline scaffolds play an important role in medicinal chemistry, especially in the identification and development of potential anticancer agents.

Cited by 106 publications

References 227 publications

Anticancer Activity of Natural and Synthetic Chalcones

Anticancer Activity of Natural and Synthetic Chalcones

Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives

Novel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design, synthesis, molecular docking studies and ADMET prediction

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