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Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues
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In the present study, five derivatives have been designed to be synthesized as possible mutual prodrugs for 5-Fluorouracil (5-FU) and non steroidal anti-inflammatory drugs (NSAIDs) to selectively deliver the drugs into the cancer cells. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC. The structure of the final compounds and their intermediates were confirmed by their melting points, infrared spectroscopy and elemental microanalysis, the hydrolysis of compound III was studied using HPLC technique. According to the results mentioned above, compounds (I−V) can be good candidates as possible mutual prodrugs of 5-FU and NSAIDs that can selectively deliver the parent drugs into the cancer cells by the effect of enzymes that elevated in tumor tissues compared with normal tissues.

Key wards: Anticancer, 5-Fluorouracil, NSAIDs, prodrug.

 

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Publication Date
Sat Jun 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Evaluation of the Possible Protective Effect of Fisetin against Cyclophosphamide-induced Genotoxicity in Bone Marrow and Spleen Cells of Male Rats
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Fisetin is a plant flavonoid found in strawberries and other fruits and vegetables such as apples, persimmons, and onions. It has many pharmacological effects like anti-inflammatory, antioxidant, cardioprotective, neuroprotective, and anti-carcinogenicity which are attributed to its ability to reduce oxidative stress which considers the main reason for different disease conditions. Genotoxicity refers to the genetic material destruction within the cell which can be caused by different chemicals as well as radiation. The present study evaluates the effect of orally-administered fisetin daily for seven constitutive days on genotoxicity induced by cyclophosphamide in rats’ bone marrow and spleen cells. Results showed that fisetin exh

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Publication Date
Mon Jul 29 2013
Journal Name
Al- Mustansiriyah J. Sci.
Synthesis and Characterization of Some Mixed Ligand Complexes of Quinaldic Acid and α-Picoline with Some Metal Salts
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Some metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato

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Publication Date
Tue Jan 01 2013
Journal Name
Al- Mustansiriyah J. Sci.
Synthesis and Characterization of Some Mixed Ligand Complexes of Quinaldic Acid and α-Picoline with Some Metal Salts
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Some metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato

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Publication Date
Thu Aug 24 2017
Journal Name
Synthesis, Characterization And Antibacterial Activity Of Mixed Ligands Complexes Of Some Metal Ions With 2-aminophenol And Tributylphosphine.
Synthesis, Characterization and antibacterial activity of mixed ligands complexes of some metal ions with 2-aminophenol and tributylphosphine
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Four metal complexes mixed ligand of 2-aminophenol (2-AP) and tributylphosphine (PBu3) were produced in aqueous ethanol with (1:2:2) (M:2-AP:PBu3). The prepared complexes were identified by using flame atomic absorption, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition antibacterial activity of the two ligands and mixed ligand complexes oboist three species of bacteria were also examined. The ligands and their complexes show good bacterial activities. From the obtained data the octahedral geometry was suggested for all prepared complexes.

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and characterization of some heterocyclic including oxazoles,Thiazoles, Pyridazines, phthalizines and Pyrazoles with evaluating of biological activity.
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A series of new compounds including p-bromo methyl pheno acetate [2]. N-( aminocarbonyl)–p-bromo pheno acetamide [3] , N-( aminothioyl) -p-bromo phenoacetyl amide [4], N-[4-(p-di phenyl)-1,3-oxazol-2-yl]-p-bromopheno acetamide [5],N-[4-p-di phenyl]-1,3-thiazol-2-yl-p-bromo phenoacet amide [6], p-bromopheno acetic acid hydrazide [7] , 1-N-(p-bromo pheno acetyl)-1,2-dihydro-pyridazin-3,6- dione [8], 1-N-(p-bromo pheno acetyl)-1,2-dihydro-phthalazin-3,8- dione[ 9], 1-(p-bromo pheno acetyl)-3-methylpyrazol-5-one [10] and 1-(p-bromo phenol acetyl)- 3,5-dimethyl pyrazole [11] have been synthesized. The prepared compounds were characterized by m.p.,FT-IR and 1H-NMR spectroscopy. Also ,the biological activity was evaluated .

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Publication Date
Thu Jun 01 2017
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis, Characterization and antibacterial activity of mixed ligands complexes of some metal ions with 2-aminophenol and tributylphosphine
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Four metal complexes mixed ligand of 2-aminophenol (2-AP) and tributylphosphine (PBu3) were produced in aqueous ethanol with (1:2:2) (M:2-AP:PBu3). The prepared complexes were identified by using flame atomic absorption, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition antibacterial activity of the two ligands and mixed ligand complexes oboist three species of bacteria were also examined. The ligands and their complexes show good bacterial activities. From the obtained data the octahedral geometry was suggested for all prepared complexes. Keywords: Mixed ligand complexes, spectral studies, 2-aminophenol, tributylphosphine.

Publication Date
Sat Oct 14 2017
Journal Name
European Chemical Bulletin
SYNTHESIS, SPECTROSCOPIC AND ANTIBACTERIAL STUDY OF ZINC, COPPER AND NICKEL COMPLEXES WITH NEW DERIVATIVE OF L-ASCORBIC ACID
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis and characterization of mixed ligand complexes of 8- hydroxy quinoline and Schiff base with some metal ions
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A new mixed ligand complexes have been prepared between 8- hydroxy quinoline and o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on with Mn(II),Fe(II),Co(II),Ni(II) and Cu(II) ions . the prepared complexes were isolated and characterized by (FT-IR)and (UV-Vis) spectroscopy. Elemental analysis (C.H.N) Flame atomic absorption technique . in addition to magnetic susceptibility and conductivity measurement.

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility
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Abstract

            Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis,  and for the prophylaxis of fungal infections in immunocompromised patients.

           The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.

          Itraconazole nanosuspension was produced by a

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Publication Date
Mon Oct 14 2019
Journal Name
Turkish Journal Of Biology
E2F6 is essential for cell viability in breast cancer cells during replication stress
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Abstract: E2F6 is a member of the E2F family of transcription factors involved in regulation of a wide variety of genes through both activation and repression. E2F6 has been reported as overexpressed in breast cancers but whether or not this is important for tumor development is unclear. We first checked E2F6 expression in tumor cDNAs and the protein level in a range of breast cancer cell lines. RNA interference-mediated depletion was then used to assess the importance of E2F6 expression in cell lines with regard to cell cycle profile using fluorescence-activated cell sorting and a cell survival assay using (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). The overexpression of E2F6 was confirmed in breast tumor cDNA samp

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