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Cephalothin as a Carrier of 6-Mercaptopurine for Targeting Cancer Tissues
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A lower extracellular pH is one of the few well-documented physiological differences between tumour and normal tissues. On the other hand, elevated glutathione (GSH) level has been detected in many tumours compared with healthy surrounding tissues. The compound II: 3-(9H-purin-6-yl-thio) carbonothionyl methyl-8-oxo-7-(2-thiophen-2-yl) acetamido-5-thia-1-azabicyclo-4-octo-ene-carboxylic acid was a cephalothin derivative contain 6-mercaptopurine (6-MP). Compound II react with general base catalysis in slightly acidic pH or with sulfhydryl nucleophiles to release the chemotherapeutic drug 6-MP. The generation of compound II was accomplished following multistep reaction procedures. The structure of compound II and its intermediate was confirmed by their melting point, infrared spectroscopy, CHN and NMR analysis. The hydrolysis of compound II in aqueous buffer solution of pH 6 and in the presence of GSH at pH 7.4 was studied. The partition coefficient (PC) of compound II was also determined. Compound II has acceptable rate of hydrolysis at slightly acidic medium pH 6 (t1/2 = 56.34 min.) and 80% of compound II had been converted to 6-MP within 30 min in the presence of GSH. And the compound has acceptable stability at pH 7.4(t0.5=639.65 min.) and the rate of hydrolysis was effected by change the buffer concentration.  This compound can selectively deliver 6-MP into the tumour tissues which have acidic pH or elevated GSH level. Compound II had an improved PC value of 12.23 compared to 1.22 for free drug 6-MP confirming higher lipophilicity.

Key words: 6-mercaptopurine, cancer, prodrug, targeting

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Publication Date
Thu Aug 01 2013
Journal Name
Desalination And Water Treatment
Competitive biosorption of Pb(II), Cr(III), and Cd (II) from synthetic wastewater onto heterogeneous anaerobic biomass in single, binary, and ternary batch systems
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Biosorption of lead, chromium, and cadmium ions from aqueous solution by dead anaerobic biomass (DAB) was studied in single, binary, and ternary systems with initial concentration of 50 mg/l. The metal-DAB affinity was the same for all systems. The main biosorption mechanisms were complexation and physical adsorption of metallic cations onto natural active functional groups on the cell wall matrix of the DAB. It was found that biosorption of the metallic cations onto DAB cell wall component was a surface process. The main functional groups involved in the metallic cation biosorption were apparently carboxyl, amino, hydroxyle, sulfhydryl, and sulfonate. These groups were part of the DAB cell wall structural polymers. Hydroxyle groups (–O

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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Synthesis, Characterization and Antibacterial Activity of 1,4-di[ aminomethylene carboxyl] phenylene (H2L) and its Complexes Co(II), Cu (II), Zn(II) and Cd (II)
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Publication Date
Fri Sep 01 2017
Journal Name
Journal Of Baghdad College Of Dentistry
In Vitro the Effect of Canals Instrumented with Three Rotary Ni-Ti Systems on the Dislocation Resistanceo Guttafusion ® versus Single Cone Obturation Technique
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Background: Complete seal of the root canal system following its chemo-mechanical debridement plays a pivotal role for achieving successful endodontic treatment. This can be established by reducing the gaps between the core filling material and root canal wall. Aim: To assess and compare the dislocation resistance of root canals obturated with GuttaFusion® and TotalFill BC sealer versus single cone obturation technique and TotalFill BC sealer after instrumentation of the canals with WaveOne, ProTaper Next and ProTaper Universal system. Material and Method: Sixty extracted human permanent mandibular premolars were conducted in the current study. The teeth were decorated and left the root with 15mm length; the roots were divided randomly i

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Publication Date
Thu Feb 28 2019
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis of some Schiff base metal complexes involving trimethoprim and 2'-amino-4-chlorobenzophenone: Spectral, thermal, DNA Cleavage antimicrobial,antifungal and Cytotoxic activity studies
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In study of effective bioactive compounds, we have synthesized the Co((ІІ), Mn(ІІ), Fe(ІІ), Cu(ІІ), Ni(ІІ), and Zn(ІІ) complexes of the Schiff base derived from trimethoprim and2'-amino-4-chlorobenzophenone and characterized by spectroscopic (NMR, IR, Mass, UV–vis,), analytical, TGA studies and magnetic data .The solution electronic spectral study suggests the stoichiometry of the synthesized complexes and Elemental analysis detected the square planer and octahedral geometry of the compounds. The prepared metal complexes presented promoted efficiency versus the screened bacterial (Escherichia Coli and Staphylococcus aureus) antibacterial efficacy against (Staphylococcus aureus, Salmonella spp., E. coli, Vibrio spp., Pseudomona

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Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
Kinetic, Isotherm, and Thermodynamic Study of Bismarck Brown Dye Adsorption onto Graphene Oxide and Graphene Oxide-Grafted-Poly (n-butyl methacrylate-co-methacrylic Acid)
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The adsorption behavior of Bismarck brown (BB) dye from aqueous solutions onto graphene oxide GO and graphene oxide-g-poly (n-butyl methacrylate-co-methacrylic acid) GO-g-pBCM as adsorbents was investigated. The prepared GO and GO-g-pBCM were characterized by Fourier transform infrared spectroscopy FTIR, which confirmed the compositions of the prepared adsorbents. Adsorption of BB dye onto GO and GO-g-pBCM was explored in a series of batch experiments under various conditions. The data were examined utilizing Langmuir and Freundlich isotherms. The Langmuir isotherm was seen as increasingly reasonable from the experimental information of dye on formulating adsorbents. Kinetic investigations showed that the experimental data were fitted ve

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Publication Date
Fri May 15 2026
Journal Name
Journal Of Physical Education
The Effect of Breathing Exercises on Relation and Self – Talk on Developing Ambition Level According to VTS – Sport and Achievement in Long Distance Runners
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Publication Date
Tue Dec 20 2022
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
FIRST RECORD OF THE LARGE-BILLED CROW CORVUS MACRORHYNCHOS WAGLER, 1827 PREDEATING ON THE VULNERABLE INDIAN ROOFED TURTLE PANGSHURA TECTA (GRAY, 1831) IN INDIA
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The Vulnerable Indian Roofed Turtle Pangshura tecta (Gray, 1831) (Testudines: Geoemydidae) occurs in the Sub-Himalayan lowlands of India, Nepal, Bangladesh, and Pakistan. Little is known about its natural history, no studies have been conducted revealing its natural predators. In this study, a group of Large-billed Crow Corvus macrorhynchos Wagler, 1827 (Passeriformes: Corvidae) was observed hunting and predating on an Indian Roofed Turtle carcass in the bank of river Kuakhai, Bhubaneswar, India. The first record of this predation behaviour is reported and substantiated by photographic evidence.

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Publication Date
Wed May 07 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
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The [2-hydroxy -1,2-diphynel-ethanone oxime] was reacted with 1,2- dichloroethan to give the new ligand [H2L].this ligand was reacted with some metal ions (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) in methanol as a solvent to give a series of new (1:1)complexes of the general formula [ M(HL)]Cl ,( where : M= Co(II),Ni(II),Cu(II),Zn(II) and Cd(II)) are isolated All compounds have been characterized by spectroscopic methods [ I.R , U.V -Vis ] atomic absorption . Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure.

Publication Date
Wed Jun 10 2015
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
New Schiff Base Derived From Folic Acid and 3- Aminoacetophenone and its Metal Complexes with Some Transition Metals and Evaluation of Their Biological Activity
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The ligand [Potassium (E)-(4-(((2-((1-(3-aminophenyl) ethylidene) amino)-4-oxo-1,4- dihydropteridin-6-yl) methyl) amino)benzoyl)-L-glutamate] was prepared from the condensation reaction of folic acid with (3-aminoacetophenone) through Schiff reaction to give a new Schiff base ligand [H2L]. The ligand [H2L] was characterized by elemental analysis CHN, atomic absorption (A.A), (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for spectroscopes), molar conductance, and melting point. The new Schiff base ligand [H2L], reacts with Mn(II), Co(II), Ni(II), Cu(II), Cr(III) and Cd(II) metal ions and (2-aminophenol), (metal : derivative ligand : 2-aminophenol) to give a series of new mixed complexes in the general formula:- K3[M2(HL)(HA)2], (where M=Mn(II) and

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Publication Date
Sun Nov 19 2017
Journal Name
Iraqi Journal Of Laser
Effects of Diode Laser 940 nm with and without 5 % Sodium Fluoride White Varnish with Tri-calcium Phosphate on Dentin Permeability (In vitro study)
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It is found that hypersensitive teeth have a larger number and wider patent tubules than those of non-sensitive teeth. Objective: The aim of this study is to compare between the effects of diode laser at different power densities, with and without sodium fluoride on the sealing of exposed dentinal tubules and dentin permeability. Materials and methods: 118 teeth were used. Samples were divided into three major groups. The first consisted of 100 teeth used for permeability test. The second consisted of 16 teeth for measuring external surface temperature elevation while irradiation. The third, in turn, consisted of one pair of teeth observed under SEM for dentine surface morphology analysis. Results: For dentin permeability measurement, th

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