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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
Sat Jan 01 2022
Journal Name
Aip Conference Proceedings
Sensitize the electrical properties of partial substitution on mercury-base superconductor manufactured by the solid reaction method
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Publication Date
Thu Feb 01 2024
Journal Name
Journal Of Engineering
Performance Evaluation of Two Stages Parallel Flow Indirect Evaporative Cooling with Aspen Pads in Baghdad Climate Conditions
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This study delves into the realm of advanced cooling techniques by examining the performance of a two-stage parallel flow indirect evaporative cooling system enhanced with aspen pads in the challenging climate of Baghdad. The objective was to achieve average air dry bulb temperatures (43 oC) below the ambient wet bulb temperatures (24.95 oC) with an average relative humidity of 23%, aiming for unparalleled cooling efficiency. The research experiment was carried out in the urban environment of Baghdad, characterized by high temperature conditions. The investigation focused on the potential of the two-stage parallel flow setup, combined with the cooling capability of aspen pads, to surpass the limitat

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Publication Date
Wed May 10 2023
Journal Name
Journal Of Engineering
Damage Detection and Assessment of Stiffness and Mass Matrices in Curved Simply Supported Beam Using Genetic Algorithm
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In this study, a genetic algorithm (GA) is used to detect damage in curved beam model, stiffness as well as mass matrices of the curved beam elements is formulated using Hamilton's principle. Each node of the curved beam element possesses seven degrees of freedom including the warping degree of freedom. The curved beam element had been derived based on the Kang and Yoo’s thin-walled curved beam theory. The identification of damage is formulated as an optimization problem, binary and continuous genetic algorithms
(BGA, CGA) are used to detect and locate the damage using two objective functions (change in natural frequencies, Modal Assurance Criterion MAC). The results show the objective function based on change in natural frequency i

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Publication Date
Wed Feb 04 2026
Journal Name
Journal Of Babylon Center For Humanities Studies
The reflection of the Arab character in Israeli children's literature in the years 1990 - 2015
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Publication Date
Thu Nov 30 2023
Journal Name
Research Journal Of Pharmacy And Technology
Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study
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Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction

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Publication Date
Fri Jan 01 2021
Journal Name
Chemosphere
Impact of anaerobically digested silver and copper oxide nanoparticles in biosolids on soil characteristics and bacterial community
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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Possible Cardio-Protective Effects of Ethanolic Artichoke Extract against 5- Fluorouracil Induced Cardiac Toxicity in Rats
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Cardiac toxicity can occur during the therapy with several cytotoxic drugs, including 5- Fluorouracil (5- FU). It is an antimetabolite that acts during the S phase of the cell cycle and is activated by thymidine phosphorylase into fluorodeoxyuridylate (5 fluoro 2'deoxyuridine 5'monophosphate, 5-FdUMP) that inhibits thymidylate synthase, thus preventing DNA synthesis that leads to imbalanced cell growth and ultimately cell death. It is still a widely used anticancer drug, since 1957. The present study aimed to evaluate the possible cardio-protective effects of ethanolic artichoke extract (Cynara scolymus L.) against 5-fluorouracil (5-FU) induced cardio-toxicity in rats by evaluating serum levels of Alanine aminotransferase, aspartate amin

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Publication Date
Sat Apr 01 2023
Journal Name
Baghdad Science Journal
Spectrophotometric Analysis of Vancomycin Hydrochloride in Pure and Pharmaceutical Injections via Batch and Cloud Point Extraction Techniques
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Development of a precise and delicate reaction has been acquired for the determination of vancomycin hydrochloride using batch and cloud point extraction (CPE) methods. The first method is based on the formation of azo dye as a result of diazotized dapsone coupled with vancomycin HCl (VAN) in a basic medium. The sensitivity of this reaction was enhanced by utilizing a nonionic surfactant (Triton X-114) and the cloud point extraction technique (second method). The azo dye formed was extracted into the surfactant-rich phase, dissolved in ethanol and detected at λmax 440 nm spectrophotometrically. The reaction was investigated using both batch and CPE methods (with and without extraction), and a simple comparison between the two

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Publication Date
Sat Apr 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Effect of Different Soil Organic Carbon Content in Different Soils on Water Holding Capacity and Soil Health
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Abstract<p>An experiment was carried out to study the effect of soil organic carbon (SOC) and soil texture on the distance of the wetting front, cumulative water infiltration (I), infiltration rate (IR), saturated water conductivity (Ks), and water holding capacity (WHC). Three levels ( 0, 10, 20, and 30 g OC kg-1 ) from organic carbon (OC) were mixed with different soil materials sandy, loam, and clay texture soils. Field capacity (FC) and permanent wilting point (PWP) were estimated. Soil materials were placed in transparent plastic columns(12 cm soil column ), and water infiltration(I) was measured as a function of time, the distance of the wetting front and Ks. Results showed that advance we</p> ... Show More
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Publication Date
Mon Jan 01 2024
Journal Name
Open Agriculture
Interannual variations of normalized difference vegetation index and potential evapotranspiration and their relationship in the Baghdad area
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Abstract<p>A monthly correlation between urban vegetation growth and potential evapotranspiration (PET) is needed for better knowledge of controlling water resources and organized irrigation processes. This study aims to explore their relationship within an urban area like Baghdad, using a linear regression model to derive a best-fit line drawn in a scatterplot on a monthly time scale. Based on two different monthly data sources: weather variables (e.g., air temperature, solar radiation, and relative humidity) and Sentinel-2 satellite imagery of 2 years, 2018 and 2021, this study presented the interannual variations of PET and normalized difference vegetation index (NDVI). The choice of these ye</p> ... Show More
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