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Synthesis and Characterization of Some New Pyridine and Pyrimidine Derivatives and Studying Their Biological Activities
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Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehyde and 2-quinoline carboxaldehyde with 4-Bromo acetophenone and 4- fluoro acetophenone respectively. Pyrimidine 13 was synthesized by reacting chalcone 11a with guanidine hydrochloride in the presence of potassium hydroxide. Pyridine derivative 14 was prepared from the reaction of chalcone 11b with ethyl cyanoacetate and ammonium acetate in glacial acetic acid. In addition, the reaction of 4-methyl benzaldehyde and 4-fluoro acetophenone with ethyl cyanoacetate and ammonium acetate in n-butanol gave pyridine derivative 16. Spectral investigations (FT-IR, 1H, and 13C-NMR) and EI-MS spectra were used to determine the structure of the prepared compounds. The synthesized derivatives were tested in vitro for their potential cytotoxicity against two different human cancer cell types, MCF-7 (breast cancer cell) or HepG2 (liver cancer cell). Compounds 5a and 14 displayed cytotoxic activity versus HepG2 cell line with IC50 values of 43.84 and 57.14 µg /mL, respectively. Furthermore, the pyridine compound 14 demonstrated cytotoxic action versus MCF-7 with an IC50 value of 50.84 g/mL. The antibacterial and anti-parasitic properties of the synthesized derivatives have also been described.

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Publication Date
Mon Jan 01 2024
Journal Name
Dyes And Pigments
3′,3′,4′,4′,5′,5′,6′,6′,6′-nonafluoro-hexyloxy groups substituted phthalocyanines: Synthesis, characterization and their biological properties
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Publication Date
Mon Jan 01 2024
Journal Name
Polski Merkuriusz Lekarski
Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
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Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w

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Publication Date
Sat Nov 01 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
SYNTHESIS, CHARACTERIZATION, THERMAL PROPERTIES, AND BIOLOGICAL EVALUATION OF AZO-TRANSITION METAL COMPLEXES
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The coupling reaction between tryptamine and 8-hydroxyquinoline led to the formation of a new azo ligand. The synthesized ligand was characterized using CHN, FT-IR, UV-Vis, and NMR spectroscopic techniques. Complexes of the ligand with VO2+, Cr3+, Mn2+, and Mo6+ ions were prepared in a (1:2) ratio, with the general formula [M(L)2]. The obtained complexes were characterized using flame atomic absorption, CHN analysis, FT-IR, and UV-Vis spectroscopy, in addition to magnetic susceptibility and conductivity measurements. The findings suggest that the ligand functions as a bidentate, with the complexes exhibiting octahedral, square planar and square pyramidal geometries. All the complexes were identified as non-electrolytes. Their antioxidant ef

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Publication Date
Wed Jul 14 2021
Journal Name
Annals Of R.s.c.b.
Synthesis, Characterization and Biological Activity of heterocyclic compounds derived from Amoxcilline drug.
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A first step in this research was to synthesize Schiff's bases(1-3)using an Amoxcilline intensification reaction with different aromatic aldehydes in absolute ethanol. In benzene and refluxing conditions,Schiff's bases were cyclized with succinic and Phthalic anhydride to give a new sequence of 1,3-oxazepine derivatives(4-6) and (7-9),respectively.The last step,cyclization reactions with sodium azide in THF solvent resulted in the formation of [10 and 11], which are supposed to be biologically significant.FT.IR, 1H-NMR and 13C-NMR (for compound 4,7,9, and 11),as well as melting points reported, were used to characterize these prepared compounds ,Bacillus (G+), Staphylococcus (G+), and E.Coli (G-)were screened against these compounds. . To i

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Publication Date
Wed Jan 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization and bioactivity study of mixed-lig and complexes with some metal ions for new dithiocarbamate,3-aminophenol
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Publication Date
Mon Jul 19 2021
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, Characterization of New Polytriazole Derivatives from Polyacryloyl chloride and Theoretical with Corrosion Inhibitor Study for Stainless steel in acidic medium
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The purpose of the study is to synthesize and characterize a new polytriazole derivative from polyacryloyl chloried, first reaction of polyacryloyl chloride with hydrazine hydrate in the presence of DMF as a solvent to obtained acid hydrazide (1) than reacted with different amide to give poly 1,2,4-triazole derivatives(1a-1c). Newly synthesized compounds were characterized by spectral methods [13C-NMR, 1H-NMR, and FTIR] and calculated some of its physical properties. Also, we worked theoretical study involving calculated the geometric configurations, total energy, dipole moment etc..,. In addition, the inhibition effect of the synthesized compounds (1a-1c) on corrosion of stainless steel in 1M HCl were studied by method of weight lo

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Publication Date
Tue Jan 01 2013
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Synthesis And Characterization Of Some New Metal Complexes Of Ethyl Cyano (2-Methyl Carboxylate Phenyl Azo Acetate)
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Complexes of (Co2+, Ni2+, Cu2+, Zn2+, Cd2+ and Hg2+) with the ligand Ethyl cyano (2-methyl carboxylate phenyl azo acetate) (ECA) have been prepared and characterized by FTIR, (UV-Visible), Atomic absorption spectroscopy, Molar conductivity measurements and magnetic moments measurements. The following general formula has been suggested for the prepared complexes [M(ECA)2]Cl2 where M = (Co2+, Ni2+, Cu2+ ,Zn2+, Cd2+, Hg2+) and the geometry is octahedral.

Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines
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A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound

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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines
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A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound

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Publication Date
Sat Jun 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis and Study the Biological Activity of Some New Pyrazole Compounds Containing 1,3,4-Oxadiazole Unite Through Vilsmeier–Haack Reaction
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