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bijps-943
Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
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Small molecules drug conjugate mutual prodrug design  (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide  bond   ;  represent new interesting approaches for cancer treatment , the component of SMDC intended  for targeting    folate receptor , along with greater conservation  of component until reaching  the target tumor tissue . The  designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were  processed forward  successfully by multistep reaction  procedures , and by Thin Layer Chromatography (TLC) for  preliminary detection of  products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI   possess optimal activity proportional with increased number of 6-MP molecules.

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Vitamin D3 on Methotrexate- Induced Jejunum Damage in Rats
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Both methotrexate and vitamin D3 are used in combination for the treatment of various diseases. The aim of this study is to highlight the effect of vitamin D3 on methotrexate-induced jejunum damage using biochemical and   histopathological  studies. Seven groups of both sexes of rats were selected and treated as follows: (Group I and Group II) : control 1,control 2 (I.P normal saline) daily for 14 and 21 days respectively ; (Group III and Group IV) :vitamin D3 groups (500 IU/rat/day) orally for 14 and 21 days, respectively;(Group V): once daily dose of methotrexate 20mg/kg, I.P injected for 4 days;(Group VI):vitamin D3 (500 IU/rat/day) once daily for 14 days and methotrexate (20 mg/kg I.P) injected only at day 10;.(Group

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Evaluation of Antimicrobial activity of several new Maleimides to Benzothiazole moiety
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In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu

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Publication Date
Sun Nov 02 2014
Journal Name
Iraqi Journal Of Pharmaceutical Science
preparation and evaluation of meloxicam microsponges as transdermal delivery system
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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Evaluation of Meloxicam Microsponges as Transdermal Delivery System
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The aim of present study was to develop gel formulation of microsponges of poorly soluble drug meloxicam (MLX) in order to enhance the release and dissolution of MLX which is the limitation for preparation in topical forms. Also skin delivery is an alternative administration for MLX that can minimize gastrointestinal (GI) side effects and improve patient compliance. The microsponges of MLX were prepared by quasi-emulsion solvent diffusion method.  The effects of drug:polymer ratio, stirring time and Eudragit polymer type on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selec

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Publication Date
Tue Jan 11 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Permeability Enhancement of Methotrexate Transdermal Gel using Eucalyptus oil, Peppermint Oil and Olive Oil(Conference Paper )#
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Abstract

Objective: the idea of this study to improve transdermal permeability of Methotrexate using eucalyptus oil, olive oil and peppermint oil as enhancers.
Method: eucalyptus oil (2% and 4%), peppermint oil (2% and 4%) and olive oil (2% and 4%) all used as natural enhancers to develop transdermal permeability of Methotrexate via gel formulation. The gel was subjected to many physiochemical properties tests. In-vitro release and permeability studies for the drug were done by Franz cell diffusion across synthetic membrane, kinetic model was studied via korsmeyer- peppas equation.
Result: the results demonstrate that safe, nonirritant or cause necrosis to rats' skin and stable till 60 days gel was successfully formulated.<

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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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Publication Date
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
The Possible Self of University Students
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The current research aims to identify the possible self of university students and the differences in the level of possible self of students in terms of gender, specialization (scientific-humanitarian), and the interaction between them. In order to achieve the objectives of the current research, the two researchers have prepared a scale of the possible self, based on the theory (Markus and Nurius, 1986). The research tool was applied to a sample of (400) male and female students who were selected through a random stratified method from Al-Mustansiriya University students/morning studies for the academic year (2019-2020). The researcher reached the following results: the research sample has a high level of possible self; there is a differ

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Publication Date
Wed Aug 19 2020
Journal Name
Revista De Chimie
Synthesis, Characterization and Biological Evaluation of Cr(III), Fe(III), Co(II), Ni(II), Zn(II) and Cd(II) Complexes Using an Azo Dye as Ligand
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Azo ligand 11-(4-methoxyphenyl azo)-6-oxo-5,6-dihydro-benzo[4,5] imidazo[1,2-c] quinazoline-9-carboixylic acid was derived from 4-methoxyaniline and 6-oxo-5,6-dihydro-benzo[4,5]imidazo[1,2-c]quinazoline-9-carboxylic acid. The presence of azo dye was identified by elemental analysis and spectroscopic methods (FT-IR and UV-Vis). The compounds formed have been identified by using atomic absorption in flame, FT.IR, UV-Vis spectrometry magnetic susceptibility and conductivity. In order to evaluate the antibacterial efficiency of ligand and its complexes used in this study three species of bacteria were also examined. Ligand and its complexes showed good bacterial efficiencies. From the obtained data, an octahedral geometry was proposed for all p

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives
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A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag

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Publication Date
Fri Nov 01 2024
Journal Name
Current Medicinal Chemistry
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR

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