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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 May 01 2021
Journal Name
Journal Of Physics: Conference Series
Study of Corrosion Inhibition for Mild Steel in Hydrochloric Acid Solution by a new furan derivative
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Abstract<p>The corrosion inhibition effect of a new furan derivative (furan-2-ylmethyl sulfanyl acetic acid furan-2-ylmethylenehydrazide) on mild steel in 1.0 M HCl was investigated using corrosion potential (ECORR) and potentiodynamic polarization. The obtained results indicated that the new furan derivative (furan-2-ylmethyl sulfanyl acetic acid furan-2-ylmethylenehydrazide) (FSFD) has a promising inhibitive effects on the corrosion of mild steel in 1.0 M HCl across all of the conditions examined. The density functional theory (DFT) study was performed on the new furan derivative (FSFD) at the B3LYP/6-311G (d, p) basis set level to explore the relation between their inhibition efficiency and molecular electro</p> ... Show More
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Publication Date
Wed Sep 01 2010
Journal Name
The International Journal Of Biochemistry &amp; Cell Biology
A plate-based assay system for analyses and screening of the Leishmania major inositol phosphorylceramide synthase
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Sphingolipids are key components of eukaryotic membranes, particularly the plasma membrane. The biosynthetic pathway for the formation of these lipid species is largely conserved. However, in contrast to mammals, which produce sphingomyelin, organisms such as the pathogenic fungi and protozoa synthesize inositol phosphorylceramide (IPC) as the primary phosphosphingolipid. The key step involves the reaction of ceramide and phosphatidylinositol catalysed by IPC synthase, an essential enzyme with no mammalian equivalent encoded by the AUR1 gene in yeast and recently identified functional orthologues in the pathogenic kinetoplastid protozoa. As such this enzyme represents a promising target for novel anti-fungal and anti-protozoal drugs. Given

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Publication Date
Thu Nov 01 2018
Journal Name
Computers &amp; Fluids
Assessing moment-based boundary conditions for the lattice Boltzmann equation: A study of dipole-wall collisions
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Publication Date
Sat Oct 22 2022
Journal Name
Aro-the Scientific Journal Of Koya University
Classification of Different Shoulder Girdle Motions for Prosthesis Control Using a Time-Domain Feature Extraction Technique
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Abstract—The upper limb amputation exerts a significant burden on the amputee, limiting their ability to perform everyday activities, and degrading their quality of life. Amputee patients’ quality of life can be improved if they have natural control over their prosthetic hands. Among the biological signals, most commonly used to predict upper limb motor intentions, surface electromyography (sEMG), and axial acceleration sensor signals are essential components of shoulder-level upper limb prosthetic hand control systems. In this work, a pattern recognition system is proposed to create a plan for categorizing high-level upper limb prostheses in seven various types of shoulder girdle motions. Thus, combining seven feature groups, w

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
A new approach for the topical treatment of acne vulgaris by clindamycin HCL supported on kalion
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Has been studied both processes Almetzaz and extortion of a substance Alklanda Maysan different amounts of Alcaúlan Guy 70% alcohol solution using the method when the wavelength

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Engineering
Efficient Energy Management for a Proposed Integrated Internet of Things-Electric Smart Meter (2IOT-ESM) System
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In this work, an efficient energy management (EEM) approach is proposed to merge IoT technology to enhance electric smart meters by working together to satisfy the best result of the electricity customer's consumption. This proposed system is called an integrated Internet of things for electrical smart meter (2IOT-ESM) architecture. The electric smart meter (ESM) is the first and most important technique used to measure the active power, current, and energy consumption for the house’s loads. At the same time, the effectiveness of this work includes equipping ESM with an additional storage capacity that ensures that the measurements are not lost in the event of a failure or sudden outage in WiFi network. Then then these measurement

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Publication Date
Wed Jun 30 2021
Journal Name
Journal Of Economics And Administrative Sciences
A proposed model for disclosing the role of the collective intelligence system in improving joint auditing
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This research aims to present a proposed model for disclosure and documentation when performing the audit according to the joint audit method by using the questions and principles of the collective intelligence system, which leads to improving and enhancing the efficiency of the joint audit, and thus enhancing the confidence of the parties concerned in the outputs of the audit process. As the research problem can be formulated through the following question: “Does the proposed model for disclosure of the role of the collective intelligence system contribute to improving joint auditing?”   

The proposed model is designed for the disclosure of joint auditing and the role

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Publication Date
Wed Mar 03 2021
Journal Name
Innovative Infrastructure Solutions
Experimental investigation of a new sustainable approach for recycling waste styrofoam food containers in lightweight concrete
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Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Nonparametric statistical study for the crime motives on a sample of inmates in Khartoum State prisons
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The aim of the research was to investigate the use of non-parametric tests in the analysis of the questionnaire and how to choose the appropriate test for testing the hypothesis of the study of crime motives in Khartoum State. The data were collected through the primary sources by designing a questionnaire and distributed to a sample of inmates in Khartoum state; the data were analysis by SPSS program using the analytical statistical method through using some of the suitable non-parametric tests for each case. The most important results of the research were: there was significant relationship between the type of crime and the age group therefore, we found that the age group (20-29) was the most frequent crime particularly, the fi

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Publication Date
Thu Jan 02 2020
Journal Name
Journal Of The College Of Languages (jcl)
The newspaper is a field for the use of phraseologism: Газета как сфера использованиея фразеологических единиц
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Idiomatic expressions in Russian journalism make one important borrowed means for making a dialogue with the receiver's intellect in so far as it has the distinct feature of  having clarity and exactness of meaning. The meaning is seen as a shortcut for covering a series of concepts and details so as to arrive at the intended meaning. This is done by stimulating the reader by the use of certain clear idioms. The use of such idioms in a journalistic text is not for a linguistic purpose only, but it is a cultural and social phenomenon reflecting the type of current changes in the society and it aims at discoursing with the reader's mind. This paper is a practi

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