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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
Mon Jun 03 2024
Journal Name
Journal Of Kufa For Chemical Sciences
Synthesis and Preliminary Biological study of New Chalcone Derivatives Containing Isoxazoline Moiety
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                          In this research work, synthesis, antimicrobial and antioxidant bioactivity of a chain of compounds having unsaturated ketones bond and isoxazoline moiety have been described. New chalcone derivatives containing isoxazoline moiety have been synthesized. Generally, Chalcones are unsaturated ketones bearing (-CO-CH=CH-) as reactive ketoethylenic group that give the bright yellow colored compounds due to this chromophore group.  Firstly, chalcones (IIa-d) have been prepared by cyclocondensation (Claisen-Schmidt condensation) of triphenyl aminobenzaldehyde with different substituted acetophenone in ethyl alcohol to produce a series of chalcones compounds with bright yellow colored as a

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Publication Date
Sat Oct 19 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity of New Ligand     Derived from 4-‎(Dimethylamino) Benzaldehyde and Nano Copper Complex
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الصيغة العامة للمعقدات الجديدة [M2(BDS)Cl4] الناتجة من تفاعل الليكاند الجديد] ن1,ن4-ثنائي(1أ –بنزو]د[ اميدازول-2-يل)-ن1,ن4-ثنائي(4-ثنائي مثيل امينو) بنزيل) سكسنمايد[ (BDS) مع الايونات الفلزية الكادميوم, الكوبلت, الزئبق, النحاس والنيكل. تم اشتقاق هذا الليكاند من تفاعل المواد الثلاث 4-(ثنائي ميثيل أمينو) بنزالدهيد، 2-أمينو بنزيميدازول، وكلوريد السكسينيل. تم تشخيص المركبات باستخدام مطيافية طيف الاشعة تحت الحمراء وطيف الرن

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization and Biological Evaluation of New Dithiocarbamate Ligand and Its Complexes with some Metal Ions
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New bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil

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Publication Date
Mon Aug 19 2024
Journal Name
Chemical Papers
In vitro and in silico evaluation of 4'-hydroxy-[1,1'-biphenyl]-4-carbohydrazide Schiff base and oxadiazole derivatives targeting EGFR allosteric site
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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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Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization of new Schiff base compounds contains 5H-thiazolo[3,4-b][1,3,4] thiadiazole and study its biological activity
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A new derivatives of Schiff bases connected with 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c were prepared via many reactions starting by treating 1,4-phenylene diamine 1 with chloroacetylchloride to prepared compound 2, then reaction with p-hydroxybenzaldehyde to synthesize compound 3 then, this was reacted with thioglycolic acid and thiosemicarazide to giveN,N-(1.4-phenylene)bis(2-(4-(2-amino-5Hthiazolo[4,3-b][1,3,4]thiadiazol-5-yl)phenoxy)acetamide) 4. Compound 4 was treated with different aromatic aldehydes to give a new derivatives of Schiff bases containing 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c. The synthesized compounds were characterized using FTIR spectrophotometer and 1H NMR spectroscopy and the biological activity of

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Publication Date
Wed Aug 03 2022
Journal Name
Chemical Methodologies
Synthesis and Characterization of New 1,3,4-Thiadiazole Derivatives Containing Azo Group from Acid Hydrazide and Studying Their Antioxidant Activity
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Various Extracts of Some Medicinal Plants as Inhibitors for Beta-lactamase Activity
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The inhibitory effect of acetone, ethanol, and aqueous extracts of ten medicinal plants on β-lactamase from Staphylococcus sciuri and Klebsiella pneumoniae was investigated in vitro by starch-iodine agar plate method. The results revealed the success of starch-iodine method for the detection of the inhibition of β-lactamase activity by the various extracts of each individual plant. The acetone extracts of Catharanthus roseus, Eucalyptus camaldulensis, and Schinus terebinthifolius induced an inhibitory effect on β-lactamase from Staphylococcus sciuri. On the other hand, acetone extracts from only Eucalyptus camaldulensis, and Schinus

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Publication Date
Fri Jun 02 2017
Journal Name
Applied Organometallic Chemistry
A new azo‐Schiff base: Synthesis, characterization, biological activity and theoretical studies of its complexes
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A new Azo‐Schiff base ligand L was prepared by reaction of m‐hydroxy benzoic acid with (Schiff base B) of 3‐[2‐(1H–indol‐3‐yl)‐ethylimino]‐1.5‐dimethyl‐2‐phenyl‐2,3‐dihydro‐1H‐pyrazol‐4‐ylamine. This synthesized ligand was used for complexation with different metal ions like Ni(II), Co(II), Pd(II) and Pt(IV) by using a molar ratio of ligand: metal as 1:1. Resulted compounds were characterized by NMR (1H and 13C), UV–vis spectroscopy, TGA, FT‐IR, MS, elemental analysis, magnetic moment and molar conductivity studies. The activation thermodynamic parameters, such as ΔE*, ΔH*, ΔS*, ΔG*and

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis of Some New Nucleoside Analogues Containing Seven Membered Ring and Studying Their Biological Activity
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In this work, a series of new Nucleoside analogues (D-galactopyranose linked to oxepanebenzimidazole moiety) was synthesized via multisteps synthesis. The first step involved preparation of two benzimidazoles 2-styrylbenzimidazole and 2-(phenyl ethynyl) benzimidazole via reaction of phenylenediamine with cinnamic acid or ?-phenyl propiolic acid. Electrophilic addition of the prepared benzimidazoles by three anhydrides in the second step afforded (4-6) and (14-16) which in turn were treated with 1,2,3,4-di-O-isopropylidene galactopyranose in the third step to afford a series of the desirable protected nucleoside analogues (7-9) ,(17-19)which after hydrolysis in methanolic sodium methoxidein the fourth step afforded the free nucleoside analog

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