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Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug
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 5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks  low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically  conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds.  ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed  enhanced cytotoxic effects for [IV] over 5-FU.

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Publication Date
Fri Jun 21 2024
Journal Name
Pharmacia
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 comp

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Publication Date
Sun Apr 02 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phosphodiester Conjugation of Metronidazole and Dexamethasone as Possible Mutual Prodrug
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As possible mutual prodrug had been synthesized that contain metronidazole and dexamethazone conjugated through phosphodiester linkage. The rationale for this type of conjugate is to get a prodrug with possible site – specific delivery of its active constituents into the lower parts of the G.I.T.

This compound was synthesized by the reaction of dexamethzone – 21 – phosphate with metronidazole to form:(1 – (dexamethazone – 21 – phosphoryl) – metronidazole)

   This conjugate was performed using dicyclohexylcarbodiimide (DCC) as a condensing agent. The identity of the prepared compound had been confirmed using T.L.C., U.V. spectroscopy, IR spectrosco

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Publication Date
Wed Jan 01 2020
Journal Name
Annals Of Tropical Medicine And Public Health
Dithiocarbamates derivatives as anticancer agents: A Review
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Publication Date
Thu Feb 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Characterization, and Study of Anticancer Activities of New Schiff Bases and 1,3-Oxazepine Containing Drug
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Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus

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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
Sat May 13 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Synthesis, Characterization of Schiff's and Mannich bases of 5-Fluoroisatin and Preliminary Antimicrobial Evaluation
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With the aim of developing potential antimicrobials, a series of new 5-fluoroisatin derivatives incorporated with different secondary amines (piperidine, morpholine, pyrrolidine, dimethylamine, and diphenylamine) for monomer, and (piperazine) in case of dimer Mannich bases, separately in presence of formaldehyde to obtain Mannich bases of 5-fluoroisatin derivatives, which then each Mannich derivatives reacts with phenylhydrazine to form Schiff bases as final products. The resulting compounds were characterized by two spectroscopic analyses; (Fourier- transform infrared) FT-IR and proton nuclear magnetic resonance spectroscopy (¹H-NMR). In addition, the in vitro antibacterial and antifungal activities were tested against some human pathogen

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Publication Date
Mon Jul 10 2023
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis and Characterization of New 1,3,4-Oxadiazole Ring on Creatinine Derivatives Using Iodine and Study Their Anticancer Effect
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Publication Date
Sun Jul 02 2023
Journal Name
Nanomedicine Research Journal
Gold and Silver Nanoparticles with Modified Chitosan /PVA : Synthesis, Study The Toxicity and Anticancer Activity
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The new novel polymers nanocomposites based modified chitosan (CS) blending with polyvinyl alcohol (PVA) and coated gold or silver nanoparticles (AuNPs), AgNPs) were synthesized from many sequence reactions as presented in (Scheme1, 2 and 3). By utilizing 1H-NMR spectroscopy, FTIR, and Field Emission Scanning electron microscope , the synthesized compounds have been identified. Molecular docking is studied, where operations are used to predict the binding status of compounds with the enzyme and to calculate the free energy (ΔG) of the compounds prepared. Also, the antibacterial activity regarding the synthesized compounds against two resistant pathogenic bacteria (G+) S. aureus and E. coli (G-) was examined in vitro compare with standard a

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Publication Date
Sun Jan 01 2023
Journal Name
Chemical Methodologies
Cytotoxicity and Anticancer Effect of Chitosan-Ag NPs-Doxorubicin-Folic Acid Conjugate on Lungs Cell Line
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This study looked at how the synthetic chitosan-AgNPs-Doxorubicin-folic acid combination affected the A549 cell line in terms of cytotoxicity and anticancer activity. By reducing silver nitrate (AgNO3) and biodegradable chitosan, silver nanoparticles were biosynthesized. The produced conjugate was examined by using FT-IR spectroscopy, atomic force microscopy (AFM), and field emission scanning electron microscopy (FE-SEM). The cytotoxicity assay for the viability of A549 cells revealed that the combination of chitosan, AgNPs, doxorubicin, and folic acid decrease cell viability in a dose-determined by method over 48 hours, which direct to a dependent reduce in the activity of A549 cells. The mechanism analysis of the impacted living cells lea

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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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