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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
Thu Jan 01 2015
Journal Name
Chemistry And Materials Research
Anticancer Activity of New Di-Nuclear Copper (I) Complex
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In-vitro biological activities of the free new H4L ( indole-7-thiocarbohydrazone) ligand and its Ni(II), Pd(II) , Pt(II), Cu(II), Ag(I), Zn(II) and Cd(II) complexes are screened against two cancerous cell lines, that revealed significant activity only for [Cu2Cl2(H4L)2(PPh3)2] after 72 h treatment by the highest tested concentrations. The Copper(I) complex was characterized by X-ray Crystallography and the NMR spectra, whereas it has been confirmed to have momentous cytotoxicity against ovarian, breast cancerous cell lines (Caov-3, MCF-7). The apoptosis-inducing properties of the Cu(I) complex have been investigated through fluorescence microscopy visualization, DNA fragmentation analysis and propidium iodide flow cytometry.

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Publication Date
Fri Oct 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Anticancer and Antioxidant activity of Gold Nanoparticles Biosynthesized using Acinetobacter baumannii
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In the current study, gold nanoparticles were made using Acinetobacter baumannii broth culture. UV-vis, FTIR, XRD, FESEM, AMF, and zeta potential measurements were also used to study the properties of the Ab-AuNPs. The average was 66 nm, ranging from 20 to 90 nm. The examination results proved that the Ab-AuNPs are semi-spherical and varied from 20 to 90 nm, with an average of 66 nm. 

   MTT assay on the breast cancer cell line MCF-7 confirmed the anticancer activity in vitro. Cancer cells showed an important cytotoxic activity of Ab-AuNPs. The breast. Cancer cell. Line.MCF-7 but ineffective against the normal.cell line.MCF-10. The IC50 values of Ab-AuNPs were at 11.45 μg ml-1. The results proved that Ab-

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Publication Date
Fri Oct 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Surface Properties of Nano-TiO2 Using a Novel Leaf Extracts
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    The main focus of research is on the nature of applications in the fields of science and technology, particularly nanotechnology. In this paper, a simple, non-toxic, inexpensive, and environmentally friendly green method was used to synthesize TiO2 nanoparticles using the extraction of portulacaria afra plant leaves and TiCl4 as a precursor. The synthesized titanium dioxide nanoparticles were characterized by scanning electron microscopy, atomic force microscopy, X-ray diffraction patterns, Fourier transform infrared spectroscopy, and Brunauer-Emmett-Teller analysis. The SEM image of TiO2 nanoparticles showed a few spherical, non-agglomerated particles. The average diameter of the nanoparticles, ac

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Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Novel Schiff Bases of Imide Moiety
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    In our research novel schiff bases of imides moiety have been synthesized . Novel Schiff base derivatives of imides moiety have been synthesized by multistep reaction . First step involves prepare 2-amino -5-mercapto-1,3,4-thiadiazole (I) by the cyclization of thiosemicarbazide with carbon disulphide and anhydrous sodium carbonate in ethanol as a solvent . Then , compound (I) was  reacted with phthalic anhydride in the presence of glacial acetic acid to give 2-(5-mercapto-1,3,4-thiadiazol-2-yl) isoindoline-1,3-dion (II).Compound (II)was heated with ethyl chloracetate in the presence of potassium carbonatproduced ethyl 2(5-(1,3-dioxoisoindoline -2-yl)-1,3,4-thiadiazole-2-yl thio) acetate (III).The reaction of compo

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Publication Date
Fri Oct 04 2024
Journal Name
Chemical Review And Letters
Newly designed 2-(aminomethyl)benzimidazole derivatives as possible tyrosine kinase inhibitors: synthesis, characterization, preliminary cytotoxic evaluation and in Silico studies
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Pharmacological Evaluation of Aminobenzensulfonamides Derivatives of Mefenamic Acid as a Potential Anti-inflammatory Agents
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A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent.  In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (c

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Publication Date
Thu Jul 18 2019
Journal Name
Annals Of Tropical Medicine & Public Health
SURVIVIN TARGETING; AN IN SILICO APPROACH FOR ANTICANCER DESIGN
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Survivin, a member of inhibitor of apoptosis family is increasingly used as a target for cancer therapy design because it has a key role in cell growth and inhibition of cell apoptosis. Also it can be used as a biomarker for targeting cancer because it is found in almost all cancer but not normal cells. Our strategy was to design (computationally) a molecule to be used as survivin inhibitor. This molecule was named lead10 and was used furthermore to find (virtually) existing drugs with a good survivin inhibition activity.

Publication Date
Sun Jun 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Antimicrobial and Antioxidant Study of New Complexes Schiff Base Derived from 2, 5-diChloroaniline
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Metal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t

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Publication Date
Thu Aug 13 2020
Journal Name
Asia Pacific Journal Of Molecular Biology And Biotechnology
The anticancer molecular mechanism of Carnosol in human cervical cancer cells: An in vitro study
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Carnosol, a phenolic diterpene, is one of the effective anticancer agents naturally occurring in rosemary, sage, parsley, and oregano. The chemoresistance problem increased with the routinely used chemotherapy. Therefore, the efforts to find a substitute with safe and low cost have become crucial worldwide. The current study attempts to inspect the anticancer molecular mechanisms of Carnosol on modulating up- and down- regulation of multiple genetic carcinogenesis pathways. The cytotoxicity of Carnosol on Hela cells was evaluated by MTS assay. Flow cytometry was used to assess apoptosis and cell cycle arrest. The apoptotic morphological changes were obvious by dual apoptosis assay. The differential gene expression after treatment wi

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Publication Date
Mon May 01 2023
Journal Name
Journal Of Medicine And Life
Mucoprotective effect of ellagic acid in 5 fluorouracil-induced intestinal mucositis model
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