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bijps-1639
Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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Abstract

A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most potent one is compound S2 (IC50: 5.73 µM). Among the tested compounds, compound S1 exhibited the highest antitumor activity against MCF-7cell line (IC50: 3.38 µM) compared to MTX (IC50: 27.32 µM). The binding modes of the synthesized compounds with the target proteins (DHFR and TS) were investigated by molecular docking studies using GOLD software.

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Publication Date
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis of Novel Porphyrin Derivatives and Investigate their Application in Sensitized Solar Cells
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Solar energy has significant advantages compared to conventional sources such as coal and natural gas, including no emissions, no need for fuel, and the potential for installation in a wide range of locations with access to sunlight. In this investigation, heterocyclic derivatives were synthesized from several porphyrin derivatives (4,4',4",4"'-(porphyrin-5,10,15,20-tetrayl) tetra benzoic acid) compound (3), obtained by reaction Pyrrole with 4-formyl benzoic acid. Subsequently, porphyrin derivative-component amides 5a, 5b, and 5c were produced by reacting compound (3) with amine derivatives at a 1:4 molar ratio. These derivatives exhibited varying sensitivities for utilization in solar cells, with compound 5a displaying the highest power

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Publication Date
Mon Jan 01 2024
Journal Name
Heliyon
Synthesis and Characterization of Some Metal Ions Complexes with Mixed Ligand of Azo Dye and Metformin and Evaluation of its Effectiveness on the Growth of Some Pathogenic Bacteria Clinically Isolated and Study of its Toxicity on Normal and Cancerous Hepatocytes
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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Four metal compounds mixed ligand of azo dye ligand (L) and metformin.(Met) were produced at aquatic ethanol for (1:1:1) (M:L:Met). The prepared compounds were identified by utilizing atomic absorption flame, FT.IR and UV–Vis spectrum manners as well as conductivity mensuration. These compounds was assayed of the gained datum the octahedral geometry was proposed into whole prepared complexes.Also in this research was studied represented examining the antibacterial and antifungal impact of the azo dye ligand (L), metformin.(Met) and (Co,Ni, Cu and Cd complexes) on four types of pathogenic, clinically isolated bacteria that are resistant to antibiotic, like Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneu

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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Publication Date
Wed Jan 29 2020
Journal Name
Advances In Rheumatology
Neutrophil/lymphocyte and platelet/lymphocyte ratios as potential markers of disease activity in patients with Ankylosing spondylitis: a case-control study
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Abstract<sec> <title>Background

The neutrophil/ lymphocyte ratio (NLR) and platelet/lymphocyte ratio (PLR) have the potential to be inflammatory markers that reflect the activity of many inflammatory diseases. The aim of this study was to evaluate the NLR and PLR as potential markers of disease activity in patients with ankylosing spondylitis.

Methods

The study involved 132 patients with ankylosing spondylitis and 81 healthy controls matched in terms of age and gender. Their sociodemographic data, disease activity scores using the Bath Ankylosing

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Publication Date
Tue Aug 01 2017
Journal Name
Journal Of Molecular Structure
Asymmetric 1,3,4-thiadiazole derivatives: Synthesis, characterization and studying their liquid crystalline properties
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Publication Date
Fri Jun 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Thermal and Biological Study of New Organic Compound with Some Metal Complexes
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A new set of metal complexes by the general formula [M(P)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-methoxyphenyl)succinamide] (P) derived from succinyl chloride with p-anisidine with the transition metal ions [Cu(II), Mn(II), Cd(II), Co(II) and Ni(II)]. Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (P)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (P) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group), and the octahedral composition of these complexes is suggested. Staphylococcus Aureus (+) and Escherichia Coli (–) were studied for the antibact

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Publication Date
Sat Dec 29 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study Biological Activity of Some New Compounds Derived From Phthalic Anhydride
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In this research , phthallic anhydride ring is opened with 4-methyl aniline and acetone as a solvent to results the compound [I] that reacted with dimethyl sulphate and anhydrous sodium carbonate formation to phathalate ester [II], while the acid hydrazide compound [III], was obtained from mixed the compound [II]with hydrazine hydrate, Synthesis four type of shiff bases[IV]a-d was synthesized from the reaction of acid hydrazide [III] with aromatic aldehyde or ketone , when reacted Shiff bases with phthalic anhydride or naphthalicanhydride,I get eight derivatives of oxazepine [V]a-d , [VI]a-d. The bacterial activity of the new compounds studied by four species of bacteria: Esherichia Coli, Enterobactecloacae (Gram negative) and staphylococcu

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