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bijps-563
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
Tue Apr 20 2021
Journal Name
Ndian Journal Of Forensic Medicine & Toxicology,
Detection Levels of Cytokines (IL-6 and IL-18) and Microbial Parameters in Patients with Renal Failure in Diyala Province
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Publication Date
Sun Sep 07 2008
Journal Name
Baghdad Science Journal
The antiviral activity of the compound chalcone (4-ethoxy-2-hydroxy-4, 6-dimethoxy-chalcone) against rubella virus in vitro
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The studies on the antiviral compound chalcone in vitro in both tissue and organ culture systems against rubella virus glass that this compound relatively non toxic to the cell culture and organ culture of the concentration of 8 ug/ml or less, chalcone have significantly antiviral activity against rubella virus in tissue culture and organ culture. We find that a concentration of 0.03ug/ml or more inhibit the IOOTCID50 of rubella virus. The therapeutic index (TI) used in this study to evaluate the drug, the (TI) which is the ratio of the dose of drug which is just toxic (Maximum tolerated dose) to the dose which is just effective (Minimum effective dose). If this index is one or less it not possible to use the drug under the conditions outli

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Publication Date
Mon Jan 01 2024
Journal Name
Clinical Laboratory
Histopathological Tracing of HPV Genotypes 6 and 11 in Pediatric Patients in Medical City with Chronic Palatine and Pharyngeal Tonsillitis
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Publication Date
Sun Sep 05 2021
Journal Name
Journal Of Arab Statistical Union (jasu)
Using Quality Control and 6-Sigma to Determine The Quality of The Treated Wastewater Discharged From Some Water Purification Plants
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Publication Date
Tue Jun 15 2010
Journal Name
International Journal Of Poultry Science
Effect of n-3 and n-6 Fatty Acid Supplemented Diets on Semen Quality in Japanese Quail (Coturnix coturnix japonica)
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Publication Date
Tue Feb 01 2022
Journal Name
Advanced Powder Technology
Functionalization of mesoporous MCM-41 for the delivery of curcumin as an anti-inflammatory therapy
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Publication Date
Tue Nov 21 2023
Journal Name
Pharmacia
A comparative study of oral diacerein and transdermal diacerein as Novasomal gel in a model of MIA induced Osteoarthritis in rats
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Background: Osteoarthritis is a chronic pathology of the joints causing disability and morbidity. Diacerein is a disease-modifying agent indicated for osteoarthritis management with enhanced performance and have much lower side effects profile than conventional non-steroidal anti-inflammatory drugs. Oral administration of Diacerein is associated with a laxative effect, thus causing treatment discontinuation. Aim: This study aimed to evaluate the activity of Diacerein novasome-based transdermal gel compared with standard oral treatment in the management of induced osteoarthritis in a rat model. Materials and methods: A single intra-articular injection of monosodium iodoacetate was administered to the left knee joint, resulting in the develop

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Publication Date
Sat Dec 01 2018
Journal Name
Al-khwarizmi Engineering Journal
A study of Land Zoning in the base of Traffic Noise Pollution Levels using ArcGIS: Kirkuk City as a Case Study
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This study is an approach to assign the land area of  Kirkuk city [ a city located in the northern of Iraq, 236 kilometers north of  Baghdad  and 83 kilometers  south of  Erbil [ Climatic atlas of  Iraq, 1941-1970  ]  into different  multi zones by using Satellite image and Arc Map10.3,  zones of different traffic noise pollutions. Land zonings process like what achieved in this paper will help and of it’s of a high interest point for the future of Kirkuk city especially urban

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Publication Date
Mon Mar 01 2021
Journal Name
Materials Today: Proccedings
Nanomaterials usage as adsorbents for the pollutants removal from waste water; areview
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Publication Date
Tue Mar 12 2019
Journal Name
Journal Of Global Pharma Technology,
Bentonite as an adsorption surface for bromothymol blue dye from aqueous solution
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