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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
Thu Jan 01 2009
Journal Name
Ibn Al- Haitha M J. Fo R Pur E & Appl. Sc I
Synthesis and Structural Study of Some Mo(II) Carbonyl Complexes with Triazole and Oxadiazole Derivatives
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A new carbonyl complexes of triazole and oxadiazole were synthesized. These complexes were identified and their structural geometric were suggested by using FT-IR and UV-Vis spectra, conductivity measurements and other chemical and physical properties. The spectra data (FT-IR, UV, Vis.) with the substantial aid of group theoretical calculations gave so many evidences for the proposed geometries and the type of bonding of these compounds

Publication Date
Thu Apr 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Polypropylene/Pt Nanocomposite: Synthesis, Characterization and Study the Cytotoxic Effects
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     This paper presents the synthesis of a polypropylene nanocomposite. The  nanocomposites were characterized using different techniques: atomic electron microscopy (AFM), surface shape was evaluated by (SEM),(EDS),(XRD) and (FTIR). The study showed that the platinum nanocomposite had a fatal effect on both strains of bacteria used, as well as on the growth of fungi. The compound tested showed antioxidant properties moderate activity was found. The mentioned material were evaluated in normal cell line HdFn (Human Dermal Fibroblasts, neonatal)  and breast cancer MCF-7 cancer cell line , by MTT assay for study cytotoxic effects, morphological changes, all experiments were conducted on cell lines by using the

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Publication Date
Mon Jun 03 2019
Journal Name
Journal Of Global Pharma Technology
New Diquinazoline Derivatives: Synthesis and Evaluation of AntiBacterial Activi
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Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf

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Publication Date
Tue Dec 29 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Antibacterial Evaluation of New Vanillic Acid Derivatives
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Publication Date
Fri May 20 2022
Journal Name
Al-kindy College Medical Journal
Potential Influence of Parasitic Diseases as Protective Agents from Infection with Pandemic COVID-19
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Parasitic diseases can affect infection with COVID-19 obviously, as protective agents, or by reducing severity of this viral infection. This current review mentions the common symptoms between human parasites and symptoms of COVID-19, and explains the mechanism actions of parasites, which may prevent or reduce severity of this viral infection. Pre-existing parasitic infections provide prohibition against pathogenicity of COVID-19, by altering the balance of gut microbiota that can vary the immune response to this virus infection.  

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Publication Date
Fri May 12 2023
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
SYNTHESIS, CHARACTERIZATION, ANTIMICROBIAL STUDIES, AND MOLECULAR DOCKING STUDIES OF TRANSITION METAL COMPLEXES FORMED FROM A BENZOTHIAZOLE-BASED AZO LIGAND
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The azo ligand obtained from the diazotization reaction of 2-aminobenzothiazole and 4- nitroaniline yielded a novel series of complexes with Co(II), Ni(II), Cu(II), and Zn(II) ions. The complexes were investigated using spectral techniques such as UV-Vis, FT-IR, 1H and 13C NMR spectroscopic analyses, LC-MS and atomic absorption spectrometry, electrical conductivity, and magnetic susceptibility. The molar ratio of the synthesized compounds was determined using the ligand exchange ratio, which revealed the metal-ligand ratios in the isolated complexes were 1:2. The synthesized complexes were tested for antimicrobial activity against S. aureus, E. coli, C. albicans, and C. tropicalis bacterial species. Additionally, their binding affinities we

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Publication Date
Mon Jun 08 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Thu Mar 19 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis, Characterization and Comparative Cytotoxic Evaluation of bis-(2- mercaptoacetate) gold (III) chloride
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In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.

With this frame, recently new square planar Au(III)  complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.

In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')

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Publication Date
Thu Apr 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
A Brief Review: Some Interesting Methods of Synthesis Chromene Derivatives as Bioactive Molecules
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Chromene is considered a fused pyran ring with a benzene ring, which is found in many plants and is part of many important compounds such as anthocyanidins, anthocyanins, catechins, and flavanones. These compounds are included under the headings "flavonoids" and "isoflavonoids." These compounds are well known as bioactive molecules with wide medicinal uses. According to these pharmacokinetic characteristics, many researchers are giving more attention to this type of compound and its derivatives. Many chromene derivatives have been synthesized to study their biological effects for the treatment of many diseases. Furthermore, the researcher displayed wide interest in finding new methods for synthesizing chromene derivatives. These met

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