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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
Mon Nov 08 2021
Journal Name
Physica Scripta
Adsorption of the eosin yellow dye by nickel oxide nanoparticles catalyzes via oxalate co-precipitation method: isotherm, kinetic and thermodynamic studies
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Publication Date
Wed Apr 01 2020
Journal Name
Biochemical And Cellular Archives
Immunohistochemical evaluation of epidermal growth factor expression in skin wound treated by capparis spinosa flavonoid extract in alloxan induced diabetes rats
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In diabetes, impaired wound healing and other tissue abnormalities are considered major concerns. Many factorsaffect the time and quality of wound healing. One of the purposes of medical sciences is wound healing in a short time withreduced side effects. The herbal products are more precious in both prophylaxis as well as curative in delayed diabetic woundhealing activity when compared to synthetic drugs.A wide range of evidence has shown that capers plant possesses differentbiological effects, including antioxidant, anticancer and antibacterial effects. Phytochemical analysis shows thatC. spinosahashigh quantities of bioactive constituents, including polyphenolic compounds, which are responsible for its health-promotingeffects. The healing

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Publication Date
Wed Dec 18 2019
Journal Name
Baghdad Science Journal
The Calculation and Analysis of the Total Electron Content Over Different Latitudes and Seasons Using the Numerical Trapezoidal and Simpson Methods
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It has been shown in ionospheric research that calculation of the total electron content (TEC) is an important factor in global navigation system. In this study, TEC calculation was performed over Baghdad city, Iraq, using a combination of two numerical methods called composite Simpson and composite Trapezoidal methods. TEC was calculated using the line integral of the electron density derived from the International reference ionosphere IRI2012 and NeQuick2 models from 70 to 2000 km above the earth surface. The hour of the day and the day number of the year, R12, were chosen as inputs for the calculation techniques to take into account latitudinal, diurnal and seasonal variation of TEC. The results of latitudinal variation of TE

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Publication Date
Tue Jan 20 2026
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Comparative Histopathological Study of Ciprofloxacin Impact on Mus Musculus Renal Cortex Infected with Multi-drug Resistance and Susceptible Uropathogenic Escherichia Coli
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Urinary tract infections are mainly caused by uropathogenic Escherichia coli, which represent a significant global issue along with the rising of antibiotic resistance and treatment challenges. The aim of this study was to evaluate ciprofloxacin efficacy as a treatment in animal models following infection with multidrug-resistant UPEC and multidrug-susceptible UPEC and to determine the nephrotoxic effect of these antibiotics on the renal cortex. Up to 76 E. coli isolates were collected from UTI patients in Baghdad province, characterized by morphological and biochemical features, and confirmed using the Vitek-2 compact system. Mice were orally infected via gastric gavage with G33 using a bacterial load of 107 cells/ml, followed by p

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Publication Date
Tue Oct 28 2025
Journal Name
Pharmacia
Association of IL-1β gene promoter polymorphisms and serum levels with etanercept response in Iraqi patients with moderate to severe psoriasis
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Psoriasis, a chronic inflammatory dermatological condition, exhibits heterogeneous responses to anti-TNF therapies such as etanercept (ETN), underscoring the need for predictive biomarkers. This study investigated the association of interleukin-1 beta (IL-1β) gene promoter polymorphisms (rs1143623 C/G, rs752338864 C/G, and rs1143627 C/T) with ETN efficacy in 80 Iraqi patients with moderate to severe plaque psoriasis. Patients were categorized according to treatment response: responders achieved ≥ 75% reduction in the Psoriasis Area and Severity Index (PASI), whereas non-responders demonstrated ≤ 50% reduction. Post-treatment serum IL-1β levels were significantly higher in non-responders (50.35 ± 15.81 pg/mL) compared to respo

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Publication Date
Mon Mar 11 2019
Journal Name
Al-khwarizmi Engineering Journal
An Investigation Study of Tool Geometry in Single Point Incremental Forming (SPIF) and their effect on Residual Stresses Using ANOVA Model
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Incremental forming is a flexible sheet metal forming process which is performed by utilizing simple tools to locally deform a sheet of metal along a predefined tool path without using of dies. This work presents the single point incremental forming process for producing pyramid geometry and studies the effect of tool geometry, tool diameter, and spindle speed on the residual stresses. The residual stresses were measured by ORIONRKS 6000 test measuring instrument. This instrument was used with four angles of (0º,15º,30º, and 45º) and the average value of residual stresses was determined, the value of the residual stress in the original blanks was (10.626 MPa). The X-ray diffraction technology was used to measure the residual stresses

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Publication Date
Mon Jun 01 2020
Journal Name
Journal Of The College Of Languages (jcl)
Structural-Semantic and Stylistic Characteristics of the New Idioms in Russian Language: Структурно-семантическая и стилистическая характеристика новых фразеологизмов русского языка
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This study is dedicated to one of the most difficult topics in Russian - this is the science of idioms. A feature of the Russian speech application in recent decades has been the effective change in the lexical composition of the Russian language. This article illustrates the semantic, grammatical and stylistic structural characteristics of the linguistic units that appeared in Russian at the end of the 20th century - the beginning of the twenty-first century. This work defines these terms : terminology, linguistic unity, and terms that are used as synonyms. In this research , we will adhere to the conciliatory view of the problem and include not only the terminology in the language units, but also the terminological compositions, saying

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Publication Date
Sat Feb 01 2020
Journal Name
Journal Of Water Process Engineering
Biochemical performance modelling of non-vegetated and vegetated vertical subsurface-flow constructed wetlands treating municipal wastewater in hot and dry climate
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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of The Mechanical Behavior Of Materials
Numerical modeling of single closed and open-ended pipe pile embedded in dry soil layers under coupled static and dynamic loadings
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Abstract<p>For the design of a deep foundation, piles are presumed to transfer the axial and lateral loads into the ground. However, the effects of the combined loads are generally ignored in engineering practice since there are uncertainties to the precise definition of soil–pile interactions. Hence, for technical discussions of the soil–pile interactions due to dynamic loads, a three-dimensional finite element model was developed to evaluate the soil pile performance based on the 1 g shaking table test. The static loads consisted of 50% of the allowable vertical pile capacity and 50% of the allowable lateral pile capacity. The dynamic loads were taken from the recorded data of the Kobe e</p> ... Show More
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Publication Date
Sat Jan 01 2022
Journal Name
International Journal Of Applied Science And Engineering
The effect of model scale, acceleration history, and soil condition on closed-ended pipe pile response under coupled static-dynamic loads
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This paper analyzes the effect of scaling-up model and acceleration history on seismic response of closed-ended pipe pile using a finite element modeling approach and the findings of 1 g shaking table tests of a pile embedded in dry and saturated soils. A number of scaling laws were used to create the numerical modeling according to the data obtained from 1 g shake table tests performed in the laboratory. The current study found that the behaviors of the scaled models, in general have similar trends. From numerical modeling on both the dry and saturated sands, the normalized lateral displacement, bending moment, and vertical displacement of piles with scale factors of 2 and 35 are less than those of the pile with a scale factor of 1 and the

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