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Synthesis and biological activity evaluation of new isatin-gallate hybrids as antioxidant and anticancer agents (in vitro) and in silico study as anticancer agents and coronavirus inhibitors
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Background: The hybrid compounds hold promise for developing novel pharmaceuticals, potentially exhibiting greater activity, mainly against viruses and cancer diseases, than their components.

Objective: In this study, researchers explored the potential synergistic effects of hybrid molecules by designing and synthesizing a series of isatin-gallate hybrids, denoted as N’-(5-substituted-2-oxoindolin-3-ylidene)-3,4,5-trihydroxybenzohydrazide (3a–d).

Methods: Isatin-gallate hybrids (3a–d) were synthesized by reacting gallic hydrazide with each of the isatin analogs (2a–d). The structures of all produced compounds were described using spectrum methods such as fourier transform infrared (FTIR), 1H-nuclear magnetic resonance spectroscopy (1H-NMR), and physicochemical attributes. The evaluation of the tested hybrids (3a–d) involved assessing their in vitro antioxidant activities using the α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method and cytotoxic activities through the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] colorimetric assay for measuring cellular growth. Furthermore, in silico analysis was applied to the final hybrids to evaluate their effects as anticancer and anti-coronavirus agents.

Conclusion: Among the examined hybrid compounds, 3b demonstrated substantial in vitro antioxidant and cytotoxic activities. In silico analysis revealed slight variations in the anticancer activity of compounds 3a–d, with differing affinities observed across various cancer cell lines. Additionally, these compounds exhibited moderate efficacy in inhibiting coronavirus activity.

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Publication Date
Fri Nov 15 2024
Journal Name
Azerbaijan Chemical Journal
EVALUATION OF ANTIOXIDANT ACTIVITY OF NOVEL ORGANOTIN COMPLEXES DERIVED FROM A NEWLY SYNTHESIZED LIGAND AND THEIR STRUCTURAL CHARACTERIZATION
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In this work, of New Ligand [(E)-5-hydroxy-4-(3-(4-methoxy phenyl) acryl amido) naphthalene -1- sulfonic acid] (ANS) was prepared by reflexing reaction of 4-amino-5-hydroxy naphthalene sulfonic acid with para methoxy cinnamic acid, this produced and described chemical was employed as ligand to prepare tri and di-organotin complexes by condensation reaction with the salts of organotin chloride (phenyl, butyl, and methyl tin chloride). Specialized methods, including elemental analysis, (tin and proton) magnetic resonance, and infrared spectra, were used to identify the complexes. DPPH (2,2-diphenyl-1-picrylhydrazyl) and CUPRAC (Cupric Reducing Antioxidant Capacity) are both commonly used methods for measuring antioxidant capacity in v

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Kinetic Study of the Hydrolysis of synthesized Ibuprofen Ester and its Biological Activity
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It is known that the oral administration of ibuprofen caused an irritation of stomach as a side effect due to its carboxylic moiety. Ibuprofen ester was synthesized by linking the carboxylic moiety of ibuprofen and the hydroxylic group of paracetamol to reduce its side effect. Study the kinetic hydrolysis of prepared ester was examined at different values of physiological pH (1.0, 5.8, 6.4 and 7.4) at 37 ± 0.1 of 1 hour period. Measurements of absorbance were carried out by UV-Visible spectrophotometer to follow the stability of ester, it showed Pseudo first order hydrolysis. The pH- apparent rate profiles of ester was exhibited a good stability at pH 1.0 and pH 5.8. Pharmacological activity in vivo of prepared ester was evaluated in re

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Publication Date
Fri Mar 29 2024
Journal Name
Iraqi Journal Of Science
Involvement of Total Antioxidant Activity and eNOS Gene rs1799983/ rs2070744 Polymorphisms in Breast Carcinogenesis
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Globally, breast cancer is the common malignancy affecting women and understanding its associated molecular events could help in disease prevention and management strategies. The present study was set to investigate an association between total antioxidant capacity (TAC) and endothelial nitric oxide synthase (eNOS) polymorphisms with breast cancer. For this purpose, 100 subjects were participated in this work, including 50 female patients diagnosed with breast cancer recruited from Oncology hospital, Baghdad - Iraq and 50 healthy women as a control group. The concentration of antioxidants was measured in the serums collected from blood samples of breast cancer patients and healthy controls. While eNOS SNPs (rs1799983, G894T and rs2070744, T

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Publication Date
Sat Aug 01 2020
Journal Name
Research Journal Of Pharmacy And Technology
Evaluation of in vivo and in vitro protective effects of quercetin on lipopolysaccharide-induced inflammation and cytotoxicology
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Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT

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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Nystatin Microparticles as a Sustained Release System
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Nystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,

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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Clinical Evaluation of Orphenadrine citrate as a Plain Tablet
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Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .

      Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .

    The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol

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Publication Date
Wed Jun 20 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antimicrobial Evaluation with DFT Study of New Two-Amino-4-(4-Chlorophenyl) Thiazole Derivatives
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2-amino-4-(4-chloro phenyl)-1,3-thiazole (1) was synthesized by refluxing thiourea with para-chloro phenacyl bromide in absolute methanol. The condensation of amine compound (1)  with phenylisothiocyanate in the presence of pyridine will  produce 1-(4-(4-chlorophenyl)thiazol-2-yl)-3-phenylthiourea(2), which is  upon treatment with 2,4 dinitrophenyl hydrazine by conventional method, afforded 1- ( 4 - ( 4 – chlorophenyl ) thiazol – 2 – yl ) – 3 - phenylhydrazonamide,N' - ( 2 , 4 -dinitrophenyl) ,(3).The characterization of the titled compounds were performed utilizing FTIR spectroscopy, 1HNMR and CHNS elemental analysis, and by me

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Publication Date
Thu Dec 15 2022
Journal Name
Journal Of Inorganic And Organometallic Polymers And Materials
Ultrasound-Assisted and One-Pot Synthesis of New Fe3O4/Mo-MOF Magnetic Nano Polymer as a Strong Antimicrobial Agent and Efficient Nanocatalyst in the Multicomponent Synthesis of Novel Pyrano[2,3-d]pyrimidines Derivatives
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Publication Date
Wed Jul 22 2015
Journal Name
Plant Growth Regulation
Effect of photosynthetic photon flux density on growth, photosynthetic competence and antioxidant enzymes activity during ex vitro acclimatization of Dieffenbachia cultivars
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Publication Date
Tue May 12 2015
Journal Name
International Journal Of Humanities, Arts, Medicine And Sciences
SYNTHESIS, SPECTRAL, DYEING PERFORMANCE AND BIOLOGICAL ACTIVITY STUDIES OF AZO DYES COMPLEXES WITH SOME METAL IONS
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Some azo compounds were prepared by coupling the diazonium salts of amines with 2,4-dimethylphenol The structure of azo compounds were determined on the basis of elemental analyses, 1HNMR, FT-IR and UV-Vis spectroscopic techniques. Complexes of nickel(II) and copper(II) have been synthesized and characterized. The composition of complexes has been established by using flame atomic absorption, (C.H.N) Analysis, FT-IR and UV-Vis spectroscopic methods as well as conductivity magnetic susceptibility measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). High molar absorbtivity of the complex solutions were observ

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