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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
Sat Mar 11 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Spectral Characterization of Some New Aromatic Schiff Bases Derivated from 2,4Dinitrophenylhydrazine
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  Four novel Schiff bases SB1 to SB4 as new aromatic compound not hydrolysed under ordinary conditions were synthesized in this study by condensation reactions between2,4dinitrophenylhydrazine: firstly with 2,4,4`-trihydroxybenzophenone to give SB1, secondly with  4hydroxybenzophenone to give SB2, thirdly with 4-dimethylaminobenzaldhyde to give SB3 and fourthly with 4-aminobenzaldehyde to give SB4. The molecular structures of these aromatic Schiff bases obtained were identified and characterized based on melting points, elemental analysis(CHN), FT-IR and UV-Visible spectra. The electronic absorption spectra of Schiff bases obtained were studied in the solvents of ethanol, DMF, water, chloroform, carbon tetrachloride and cyclohe

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Publication Date
Sun Apr 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis And Characterization Of New Metals Complexes Of [N-(acetyl amino) Thioxomethyl] Valine
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A new ligand [N-(acetyl amino) thioxomethyl] valine was prepared from the reaction of acetyl iso thiocyanate with valine. The ligand was characterized by FT-IR, UV- vis and 1HNMR spectrum, The complexes with some metal ions (M +2 =Co,Ni,Cu,Zn,Cd,Hg) have been prepared and characterized. The structural diagnosis were established by IR,UV-Vis  spectrum, flame atomic absorption spectroscopy conductivity and magnetic susceptibility ,the complexes showed tetrahedral geometry around the metal   l.

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Publication Date
Tue Nov 30 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of a Nano (CdO)0.94:(In2O3) 0.06 / Si gas Sensor
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In this work, a (CdO)0.94:(In2O3)0.06 film was developed on a glass substrate using Q- switching pulse laser beam (Nd:YAG; wavelength 1064 nm). The quantitative elemental analysis of the (CdO)0.94:(In2O3)0.06 thin film was achieved using energy dispersive X- ray diffraction (EDX). The topological and morphological properties of the deposited thin film were investigated using atomic force microscope (AFM) and field emission scan electron microscopy (FESEM). The I-V characteristic and Hall effect of (CdO)0.94 :(In2O3)0.06 thin films were used  to  study the electrical properties. The gas sensor prope

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Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Properties of Trimethylolpropane Triesters from Coconut (Cocos nucifera) Methyl Esters
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In this study, the acid-alkaline transesterification of refined coconut seed oil (RCOSO) to fatty acid methyl ester was followed by the production of a trimethylolpropane-based thermosensitive biolubricant using potassium hydroxide, and its physicochemical characteristics were evaluated. The American Standard Test for Materials (ASTM) was employed to ascertain the biolubricant's pour point and index of viscosity, which were found to be -4 oC and 283.75, respectively. The opposite connection between lubricant viscosity and temperature was shown by the measured viscosities at varied transesterification to be transformed into biodiesel. Following this, a biolubricant was created by further transesterifiedtemperature. The ester gr

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Publication Date
Tue Feb 28 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of New Bis-Schiff Bases Linked to Various Imide Cycles
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       This research includes the synthesis of new bis-Schiff bases linked to different imide cycles. There were some steps involved in the synthesis of the novel Schiff bases with succinimide, phthalimide, tetrachlorophthalimide, and tetrabromophthalimide cycles. The first step involved the preparation of 4,4`-bis[(4-aminophenyl) methyl benzylidene]tolidine (1) via the condensation reaction of 3,3'-dimethyl-(1,1'-biphenyl)-4,4'-diamine with 4-amino acetophenone. In the second step, compound 1 reacted with various cyclic anhydrides, affording bis-amic acid Schiff bases 2-5. In the third step, the products 2-5 were dehydrated using the fusion method to prod

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Publication Date
Thu Jan 01 2015
Journal Name
Der Pharma Chemica
Synthesis, characterization and biological evaluation of new potentially active hydrazones of naproxen hydrazide
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To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap

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Scopus
Publication Date
Sun Apr 06 2008
Journal Name
Diyala Journal For Pure Science
Preliminary Test Bayesian –Shrunken Estimators for the Mean of Normal Distribution with Known Variance
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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)
Design and Synthesis of Some Nitrate Derivatives of Mefenamic Acid with Expected Nitric Oxide Release
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This study include design and synthesis of 2 derivatives of compounds consisting of mefenamic acid, glycine and organic nitrates (2-nitrooxy ethanol or 1,3-dinitrooxy-2-propanol). Nitric oxide NO has been reported to support many of the same mucosal protection mechanisms as prostaglandins and is sufficient for acute gastroprotection and ulcer healing. So we suppose these 2 compounds would reduce non-steroidal anti-inflammatory drugs NSAIDs gastrointestinal side effect.

Key words: Non-Steroidal anti-inflammatory dr

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Crossref
Publication Date
Fri May 01 2020
Journal Name
Systematic Reviews In Pharmacy
Methotrexate effect on obestatin, progranulin and kidney function in RA Iraqi males patients
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Methotrxate (MTX) has become the standard of care and first-line therapy for patients who have RA and consider as a gold standard of treatment for RA. The role of MTX in the treatment of RA has now been well established. The use of MTX treatment of RA inhibits proliferation of the lymphocytes, reduces signs and symptoms this disease, reduces progression damage of the joints and improves quality of life outcome. Progranulin (PGRN) acts a role in autoimmune inflammatory, has important function in several processes including immune response. Present study has conducted to find the effect of MTX drugs as a therapeutic target for RA patients because of its ability to bind with tumor necrosis factor receptor (TNFR), with progranulin, obestatin an

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Scopus
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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