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bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple  drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed  towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of  two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis  of the target compounds was  accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed  that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug  selectively  into the cancer cells to be hydrolyzed by enzymes that are elevated in  tumor tissues compared with normal tissues .

Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Characterization of the Groundwater within Regional Aquifers and Suitability Assessment for Various Uses and Purposes-Western Iraq
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Groundwater quality investigation has been carried out in the western part of Iraq (west longitude '40°40). The physicochemical analyses of 64 groundwater samples collected from seven aquifers were used in the determination of groundwater characterization and assessment. The concept of spatial hydrochemical bi-model was prepared for quantitative and qualitative interpretation. Hydrogeochemical data referred that the groundwater is of meteoric origin and has processes responsible for observed brackishness. The geochemical facies of the groundwater reveal that none of the anions and cations pairs exceed 50% and there are practically mixtures of multi-water types (such as Ca–Mg–Cl–HCO3 and Na+K–SO4–Cl water type) as do

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Publication Date
Fri Mar 01 2024
Journal Name
Construction And Building Materials
Uni- and tri-axial tests and property characterization for thermomechanical effect on hydrated lime modified asphalt concrete
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Permanent deformation, fatigue and thermal cracking are the three typical distresses of flexible pavement. Using hydrated lime (HL) into the conventional limestone mineral additive has been widely practiced, including in Europe, to improve the mechanical properties of hot mix asphalt (HMA) concrete and as the result the durability of the constructed pavement. Large number of experimental studies have been reported to find the optimum addition of HL for the improvement on HMA concrete mechanical properties, moisture susceptibility and fatigue resistance. Pavement in service is under complex thermomechanical stress-strain conditions due to coupled atmospheric and surrounding environment temperature variation and the traffic loading. To predic

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Publication Date
Wed Jan 01 2020
Journal Name
European J Ournal Of Molecular & Clinical Medicine
Synthesis, Characterization and Antibacterial Evaluation of Mixed Ligand Complexes of 2-phenyl-2-(o-tolylamino) Acetonitrile and Histidine ligand with Co, Cu, Zn divalent Metal Ion Complexes
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Anew mixed compound complexes derived from 2-phenyl-2-(o-tolylamino) Acetonitrile as primary ligand (L1) and histidine (L2) as secondary ligand have been prepared and characterized by conventional techniques, elemental microanalysis (C.H.N), Fourier transform infrared, ultra violet-visible spectra, , flame atomic absorption, molar conductivity, magnetic susceptibility measurement and 1H-NMR spectra. From IR data which appear chelating behavior of the amino acid ligand (L2) toward transition metal ions is via carboxylate oxygen, amino nitrogen and imidazol nitrogen as tridentate ligand while second ligand (L1) chelating through N-nitrile and N-aniline, according to all above technics the octahedral shapes were expected for these complexes as

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis & Characterization of Oxazinan and 5-oxa-7-aza-spiro[2,5] octane from reaction of Dibenzylidene with malonic anhydride and 5-oxa-spiro[2,3] hexane-4,6-dione.
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Di Benzylidenes were prepared by condensation of 1,2-diamino benzene with o- hydroxy benzaldehyde. These dibenzylidenes when treated with one equivalent of malonic anhydride or 5-oxo-spiro[2,3]hexane-4,6-dione in dry benzene give 6-membered heterocyclic ring system of 3-{2-[(2-Hydroxy-benzylidene)-amino]-phenyl}-2-(2-hydroxy –phenyl)-[1,3]oxazinane-4,6-diones ( 1-3) or 7-{2-[(2-hydroxy-benzylidene)-amino]-phenyl}-6-(2-hydroxy-phenyl)-5-oxa-7-aza-spiro[2.5]octane-4,8-diones ( 7- 9 ) But when two equivalents of malonic anhydride or 5-oxo-spiro[2,3]hexane-4,6-dione were used and under sam conditions compounds (4-6 , 10-12 ) were obtained .

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Publication Date
Tue Sep 24 2019
Journal Name
Journal Of Petroleum Research And Studies
Lithofacies Characterization of the Early – Middle Miocene Succession, Case-Study, South Iraq
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The Early – Middle Miocene Ghar and Lower Fars sedimentary succession at the representative oil-well Nu-18 of the Nahr Umr oil field south Iraq; is taken by this study to investigate the sedimentological to reservoir rock facies buildups and related reservoir zonation; as first rock-typing attempt for the both formations. The sedimentological characterization of the Early Miocene Ghar formation is mainly comprised by successive buildups of sands-gravels and sandstones, whereas; the Middle Miocene Lower Fars formation is started by limestone, limestone-marly/marl anhydritic, upgraded into interbedded-series of marl and anhydrite facies, with less-common occurrences of thin-sandstone interlayers, terminated by marl-sandy-secti

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Publication Date
Thu Sep 27 2012
Journal Name
Journal Of Physiological And Biomedical Sciences
The promising anticancer efficacy of parsley seeds flavonoid (apigenin) in induced mammary adenocarcinoma (AMN3) mice
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Extraction and identification of parsley (Petroselinum sativum) seeds flavonoids (apigenin), as well as evaluation its anticancer efficacy was the main aim of the current study. Thin layer chromatography results clarified that apigenin is the major flavonoid in parsley seeds. The cytotoxic effect of apigenin in mammary adenocarcinoma (AMN3) bearing mice was manifested through significant (P ≤ 0.01) reduction in tumor volume and growth rate inhibition (90.8 %) after 24 days of oral administration at a dose of 300 mg/kg body weight. The volume of tumor in the treated group reached 1354.8 mm³ while the recorded size of the control was 14758 mm³. Transplanted cancer mice showed a significant (P ≤ 0.01) elevation in concentration of liver,

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Publication Date
Wed Jun 21 2017
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis and characterization of Mixed-Ligand Complexes of Oxalic Acid and Trimethoprim with Mn(II), Co(II), Ni(II), Cu(II),Zn(II), and Cr (III) Ions: and antimicrobial Activities
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Publication Date
Tue Feb 27 2024
Journal Name
Pharmacia
Association of the rs1801133 and rs1801131 polymorphisms in the MTHFR gene and the adverse drug reaction of methotrexate treatment in a sample of Iraqi rheumatoid arthritis patients
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Background: Methotrexate is one of the mainstays for treating rheumatoid arthritis (RA) with a wide range of adverse drug reactions, however, it’s the relationship between adverse drug reactions and genetic polymorphism remains to be highlighted, and there is a lack of studies concerning Arabic Iraqi population regarding this aspect.

Objective: Evaluate the association between genetic mutations in the MTHFR gene in SNPs (rs1801133G>A and rs1801131T>G) on the adverse drug reaction for RA Iraqi patients.

Methods: An observational study, that involved 95 Iraqi RA patients with established RA. Patien

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Antimicrobial Study of Possible Mutual Prodrugs of Amoxicillin and Metronidazole by Direct and Indirect Coupling through Spacer
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Amoxicillin have been conjugated with metronidazole as possible mutual prodrug to get a wider spectrum of activity by acting on aerobic and anaerobic bacteria, have antifungal activity, to provide protection for beta lactam ring of amoxicillin and also to improve patient compliance as it given as a single dose therapy. The structures of the synthesized compound were confirmed and characterized using elemental microanalysis (CHN), IR and some physiochemical properties. Biological study was done by using  disc diffusion method against different bacterial strains which are , Staphylococcus aureus , Salmonella typhie , Pseudomonas aeruginosa , E. coli , Klebsiella pneumonia and fungi ( Candida albicans) . using nutrien

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Publication Date
Wed Apr 07 2010
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Spectral Studies for new Schiff base and its Binuclear Complexes with ZnII,CdII and HgII
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A new ligand (H4L) and its complexes with ( ZnII, CdII and HgII) were prepared. This ligand was prepared in two steps. In the first step a solution of terephthaldehyde in methanol was reacted under reflux with 1,2-phenylenediamine to give an precursor compound which reacted in the second step with 2,4-dihydroxybenzaldehyde to give the ligand. The complexes were then synthesized by direct reaction of the corresponding metal chloride with the ligand. The ligand and complexes were characterized by spectroscopic methods FT-IR, UV-Vis, 1 HNMR, and atomic absorption, chloride content, HPLC, mole-ratio determination. in addition to conductivity measurement. The data of these measurements suggest a distorted tetrahedral geometry for ZnII, C

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