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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
Sat Jan 01 2022
Journal Name
Pharmacia
Synthesis, docking study, and structureactivity relationship of novel niflumic acid derivatives acting as anticancer agents by inhibiting VEGFR or EGFR tyrosine kinase activities
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Publication Date
Fri Sep 02 2022
Journal Name
Military Medical Science Letters
SOLID LIPID NANOPARTICLES AS A PROMISING APPROACH FOR DELIVERY OF ANTICANCER AGENTS: REVIEW ARTICLE
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Cancer disease has a complicated pathophysiology and is one of the major causes of death and morbidity. Classical cancer therapies include chemotherapy, radiation therapy, and immunotherapy. A typical treatment is chemotherapy, which delivers cytotoxic medications to patients to suppress the uncontrolled growth of cancerous cells. Conventional oral medication has a number of drawbacks, including a lack of selectivity, cytotoxicity, and multi-drug resistance, all of which offer significant obstacles to effective cancer treatment. Multidrug resistance (MDR) remains a major challenge for effective cancer chemotherapeutic interventions. The advent of nanotechnology approach has developed the field of tumor diagnosis and treatment. Cancer nanote

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
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         A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50

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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
In silico analysis of quercetin as potential anti-cancer agents
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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Coumarin Derivatives Coupled to Amino Acid Esters and Studying their Biological Activity as Antimicrobial Agents
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A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents
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In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moder

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Publication Date
Sun Dec 01 2019
Journal Name
Baghdad Science Journal
Extraction, Purification and Characterization of Peroxidase from Pseudomonas aeruginosa and Utility as Antioxidant and Anticancer
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        Peroxidase is a class of oxidation-reduction reaction enzyme that is useful for accelerating many oxidative reactions that protect cells from the harmful effects of free radicals. Peroxidase is found in many common sources like plants, animals and microbes and have extensive uses in numerous industries such as industrial, medical and food processing. In this study, P. aeruginosa was harvested to utilize and study its peroxidases. P. aeruginosa was isolated from a burn patient, and the isolate was verified as P. aeruginosa using staining techniques, biochemical assay, morphological, and a sensitivity test. The gram stain and biochemical test result show rod pink gram-ne

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Publication Date
Wed Apr 01 2020
Journal Name
Biochemical & Cellular Archives
SYNTHESIS, CHARACTERIZATION, ANTIOXIDANT, ANTICANCER HUMAN STUDIES AND BIOLOGICAL ACTIVITY OF MIXED LIGAND COMPLEXES USING SCHIFF BASE LIGAND AND HISTIDINE.
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الوصف Mixed ligand complexes of Cu (II), Co (II) and Zn (II) with 2-((4-(1-(4-chlorophenylimino) ethyl) phenylimino) methyl) phenol (L) and histidine (His) have been prepared and diagnosed by ¹H and13 C NMR, FT-IR and electronic spectral data, thermal gravimetric, molar conductance and metal analysis measurements. The ligand (L) shows a bidentate nature and the coordination occurs through N and O atoms of imine group and phenol group respectively whereas (His) behave as tridentate ligand, coordinating through the-NH2 group and carboxylate oxygen group and N atoms of imidazole ring. The analytical studies for three complexes have shown octahedral structure. The anticancer activity was screened against human cancer cell such Follicular

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Publication Date
Fri Aug 18 2023
Journal Name
Medicinal Chemistry Research
New tolfenamic acid derivatives with hydrazine-1-carbothioamide and 1,3,4-oxadiazole moieties targeting VEGFR: synthesis, in silico studies, and in vitro anticancer assessment
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Publication Date
Mon May 30 2022
Journal Name
Egyptian Journal Of Chemistry
Design ,Synthesis, Insilco Study and Biological Evaluation of New Coumarin-Oxadiazole Derivatives as Potent Histone Deacetylase Inhibitors
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