A Review of Chalcones: Synthesis, Reactions, and Biological Importance

Mukhtar, Shorouk S.; Morsy, Nesrin M.; Hassan, Ashraf S.; Hafez, T. S.; Hassaneen, Hamdi M.; Saleh, Fatma M.

doi:10.21608/ejchem.2022.112735.5125

Cited by 5 publications

(6 citation statements)

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“…This showed that some metal complexes had better activities in comparison with the original Schiff base ligand. [ 45,46 ] In comparison with screening of another previous new synthesized ferrocene‐based Schiff base ligand HL from condensation of 2‐aminophenol with 2‐acetylferrocene and its three lanthanide metal complexes (La(III), Er(III), and Yb(III)), [ 38 ] against four bacterial strains P. aeruginosa (G + ) and E. coli (G + ) and pneumoniae (G − ) and B. subtilis (G − ). The antibacterial activities were observed that La(III) complex showed strong biological activities of inhibition zone diameter in the range of 10–19 mm/mg.…”

Section: Resultsmentioning

confidence: 99%

Bioactive La(III), Er(III), Yb(III), Ru(III), and Ta(V) complexes of new organometallic Schiff base: Preparation, structural characterization, antibacterial, anticancer activities, and MOE studies

Deghadi

Mohamed

Mahmoud

2022

Applied Organom Chemis

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Bioactive complexes [La(L)(H 2 O) 3 Cl]Cl 2 .2H 2 O (1), [Er(L)(H 2 O) 3 Cl]Cl 2 (2), [Yb (L)(H 2 O) 2 Cl 2 ]Cl.4H 2 O (3), [Ru(L)(H 2 O) 2 Cl 2 ]Cl.H 2 O (4), and [Ta(L)(H 2 O)Cl 5 ](5) have been prepared from 2-acetylferrocene derivative Schiff base (L) and characterized with different spectroscopic tools. Infrared (IR) spectral data proved the action of the ligand as a neutral bidentate Schiff base, coordinating via N-azomethine and N-pyrazole. Ta(V)-complex was eight-coordinated complex, whereas others were six-coordinated complexes. Molar conductance results showed that La(III) and Er(III) chelates were 1:2 electrolytes, Yb(III) and Ru(III) chelates were 1:1 electrolytes, and Ta(V) chelate was non-electrolyte. Thermal behavior of all compounds was characterized by thermogravimetric analysis/differential thermogravimetric analysis (TG/DTG) curves with mass loss related to dehydration, coordination, and decomposition steps. Growth inhibitory effect and IC 50 values of compounds toward MCF-7 cancer cell line were measured, and the data revealed that all complexes showed higher anticancer activity than free ligand. The lowest IC 50 value was 4.5 μg/mL for La(III) and Ru(III) complexes. Furthermore, almost complexes showed good activities against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus species with inhibition zone diameter in the range of 10-15 mm/mg. While, they had no antifungal activities against Candida albicans and Aspergillus flavas species. Finally, the strong binding affinity of ligand and its complexes with different protein receptors was confirmed by MOE studies.

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Section: Resultsmentioning

confidence: 99%

Bioactive La(III), Er(III), Yb(III), Ru(III), and Ta(V) complexes of new organometallic Schiff base: Preparation, structural characterization, antibacterial, anticancer activities, and MOE studies

Deghadi

Mohamed

Mahmoud

2022

Applied Organom Chemis

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“…Chalcones and their skeletal system widely exist in many natural compounds and are a very attractive tool for the synthesis of different heterocyclic compounds. [1][2][3] Chalcones show various biological activities such as antioxidant, [4,5] antimicrobial, [6,7] antiinfammatory, [8] antihypertensive, [9] antihistaminic, [10] anticancer. [11] Thiophene-based chalcones also show many biological activities such as antibacterial, [12] anticancer (Figure 1, compound 1), [13] and enzyme inhibition (Figure 1, compound 2).…”

Section: Introductionmentioning

confidence: 99%

“…Chalcones and their skeletal system widely exist in many natural compounds and are a very attractive tool for the synthesis of different heterocyclic compounds [1–3] . Chalcones show various biological activities such as antioxidant, [4,5] antimicrobial, [6,7] anti‐infammatory, [8] antihypertensive, [9] antihistaminic, [10] anticancer [11] .…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Characterization, Enzyme Inhibition, Molecular Docking, and Pharmacological Evaluation of New Chalcone‐Sulfonate Derivatives Bearing Thiophene

Aslan,

Yetişsin,

Korkmaz

et al. 2024

ChemistrySelect

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The novel chalcone‐sulfonate derivatives bearing thiophene motif were synthesized and characterized using 1H NMR, 13C NMR, and HRMS analysis. The evaluation of in vitro and in silico potential pancreatic lipase inhibition activity of the novel chalcone‐sulfonate derivatives bearing thiophene motif was scanned. IC50 values of compounds 5 i (28.76±2.11 μM) and 5 f (30.58±0.45 μM) were determined to be more effective pancreatic lipase inhibitors for in vitro studies. The best potential inhibitor for pancreatic lipase binding affinity was found as compound 5 f (−9.8 kcal mol−1) for in silico studies. Although compounds 5 f and 5 i were identified as the best pancreatic lipase inhibitor candidates in vitro and molecular docking studies, compounds 5 f and 5 i were predicted mutagenic and carcinogenic properties in mice according to ADMET studies. Deeply, compound 5 h was a more effective pancreatic lipase inhibitor according to enzyme inhibition, molecular docking, and ADMET studies. It can be said that compound 5 h may be a more efficient drug candidate than orlistat in the treatment of obesity.

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“…Some of these ligands were found to be non-malignant in combination with copper complex by Ames test, 26 while other Schiff bases were predicted to be mutagenic. 27 Aromatic aldehydes have an effective conjugation system, and therefore are more stable than aliphatic ones. 28 4-(dimethylamino) benzaldehyde is one of the aromatic aldehydes that were shown to have biological activity.…”

Section: Introductionmentioning

confidence: 99%

“…The mutagenic and carcinogenic potential of many Schiff bases has been previously studied. Some of these ligands were found to be non‐malignant in combination with copper complex by Ames test, 26 while other Schiff bases were predicted to be mutagenic 27 . Aromatic aldehydes have an effective conjugation system, and therefore are more stable than aliphatic ones 28 .…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial screening involving Helicobacter pylori of nano‐therapeutic compounds based on the amoxicillin antibiotic drug

Hassan,

Nader,

Nagy

et al. 2023

Helicobacter

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Nano‐structure Cu(II) complex [Cu(AMAB)2]Cl2 with Schiff base (AMAB) derived from the condensation between 4‐(dimethylamino)benzaldehyde and amoxicillin trihydrate was prepared. (AMAB) Schiff base and its Cu(II) complex were identified and confirmed by different physicochemical techniques. The Schiff base (AMAB) was coordinated to copper ion through carbonyl oxygen and imine nitrogen donor sites. X‐ray powder diffraction shows a cubic crystal system of the Cu(II) complex. The density functional theory was used to optimize the structure geometries of the investigated compounds. The molecular docking of the active amino acids of the investigated proteins' interactions with the tested compounds was evaluated. The bactericidal or bacteriostatic effect of the compounds was screened against some bacterial strains. The activity of Cu‐chelate against Gram‐negative bacteria was mainly more effective than its (AMAB) ligand and vice versa in the case of Gram‐positive bacteria. The biological activity of the prepared compounds with biomolecules calf thymus DNA (CT‐DNA) was determined by electronic absorption spectra and DNA gel electrophoresis technique. All studies revealed that the Cu‐chelate derivative exhibited better binding affinity to both CT‐DNA than the AMAB and amoxicillin itself. The anti‐inflammatory effect of the designed compounds was determined by testing their protein denaturation inhibitory activity spectrophotometrically. All obtained data supported that the designed nano‐Cu(II) complex with Schiff base (AMAB) is a potent bactericide against H. pylori, and exhibits anti‐inflammatory activity. The dual inhibition effects of the designed compound represent a modern therapeutic approach with extended spectrum of action. Therefore, it can act as good drug target in antimicrobial and anti‐inflammtory therapies. Finally, H. pylori resistance to amoxicillin is absent or rare in many countries, thus amoxicillin nanoparticles may be beneficial for countries where amoxicillin resistance is reported.

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A Review of Chalcones: Synthesis, Reactions, and Biological Importance

Cited by 5 publications

References 0 publications

Bioactive La(III), Er(III), Yb(III), Ru(III), and Ta(V) complexes of new organometallic Schiff base: Preparation, structural characterization, antibacterial, anticancer activities, and MOE studies

Bioactive La(III), Er(III), Yb(III), Ru(III), and Ta(V) complexes of new organometallic Schiff base: Preparation, structural characterization, antibacterial, anticancer activities, and MOE studies

Design, Synthesis, Characterization, Enzyme Inhibition, Molecular Docking, and Pharmacological Evaluation of New Chalcone‐Sulfonate Derivatives Bearing Thiophene

Antimicrobial screening involving Helicobacter pylori of nano‐therapeutic compounds based on the amoxicillin antibiotic drug

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