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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
Tue Mar 03 2020
Journal Name
Molecular Biology Reports
Correlation of GSTP1 gene variants of male Iraqi waterpipe (Hookah) tobacco smokers and the risk of lung cancer
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Glutathione-S-transferases (GSTs) play a role in the detoxification of environmental chemicals and mutagens, such as those inhaled during tobacco smoking. There have been conflicting reports concerning GST polymorphisms as risk factors in the development of lung cancer. No studies focused on Arab populations exposed to Waterpipe (WP) tobacco smoke have been undertaken. Here Polymerase Chain Reaction-Restriction Fragment Length Polymorphism (PCR-RFLP) and gene sequenc- ing were applied to analyze allelic variations in GSTP1-rs1695 and -rs1138272 amongst 123 lung cancer patients and 129 controls. The data suggest that WP smoking raised the risk of lung cancer more than three-fold (OR 3.6; 95% CI 2.1–6.0; p < 0.0001). However, there was no s

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Publication Date
Sat Apr 01 2017
Journal Name
2017 International Conference On Environmental Impacts Of The Oil And Gas Industries: Kurdistan Region Of Iraq As A Case Study (eiogi)
Inverse fluidized bed for chromium ions removal from wastewater and produced water using peanut shells as adsorbent
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Publication Date
Fri Apr 01 2022
Journal Name
Desalination And Water Treatment
MgCl2 and MgSO4 as draw agents in forward osmosis process for East Baghdad oilfield produced water treatment
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This study investigated a novel application of forward osmosis using different types of draw solutions for oilfield produced water treatment from the East Baghdad oilfield affiliated to the Midland Oil Company (Iraq). Magnesium chloride (MgCl2) and magnesium sulfate (MgSO4) were used as draw solutions in forward osmosis process to evaluate their effectiveness. Experiments were conducted in a laboratory scale forward osmosis system with cellulose triacetate hollow fiber membrane. In this work, sodium chloride solution was used as a feed solution with a concentration of 76 g/L (same concentration as the East Baghdad oilfield produced water) and the applied external pressure on the feed solution side was 2 bar. The impact of draw solution (DS)

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Publication Date
Sun Jan 01 2017
Journal Name
Medical Journal Of Babylon
His- Ventricle (HV) Interval And Syncope As Predictor For Pacemaker Implantation In Patients With Bifascicular Block (BFB)
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Transient drop in the heart beat or transient heart block (AVB) may be consider the main cause of syncope or presyncope inpatients with bifascicular block and syncope According to the Guidelines for cardiac pacing pacemaker consider part of treatment. Aims of our study were to evaluate whether there is role for EPS in patients BFB and to evaluate the symptoms after pacing. 42 patients were enrolled in this study, with mean age value (63.4± 12.2years), suffer from interventricular conductive defect and syncope; patients underwent EPS on admission time, and pacemaker implantation accordingly and programmed follow up for the device in the last four years. Our patients were 25 (59.5%) male and 17 (40.5%)female, all of them with syncope o

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Aquatic Oligochaeta (Annalida:Clitellata) as Bio Indication for Sediment Quality Assessment in Tigris River Within Baghdad City /Iraq
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Aquatic Oligochaeta is an important group of Macroinvertebrates that has been very remarkable as bioindicators for assessing water pollution and determining its degree in water bodies. Hence, the idea of the current study aims at studying the impact of Baghdad effluents on the Tigris River by using oligochaetes community as bioindicators . For this purpose, four sites along the inside of Baghdad has been chosen. Site S1 has been located upstream, site S2 and S3 has been at midstream and site S4 at the downstream of the River.This investigation has used different types of biological indicators, including the  percentage of oligochaeta  within benthic invertebrates, which ranged from 49.2-51.28%. The highest percentage of the tubificid w

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Publication Date
Mon Oct 27 2014
Journal Name
Desalination And Water Treatment
Simultaneous adsorption–precipitation characterization as mechanisms for metals removal from aqueous solutions by cement kiln dust (CKD)
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Publication Date
Tue Aug 01 2017
Journal Name
Iosr Journal Of Dental And Medical Sciences (iosr-jdms)
Is deferasirox As Effective As Desferrioxamine in Treatment of Iron Overload In Patients With Thalassemia Major?
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Publication Date
Wed Jan 01 2020
Journal Name
Gastric And Breast Cancer
The 21-gene oncotype DX offers more accurate treatment decisions in early breast cancer
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Publication Date
Wed Feb 01 2023
Journal Name
Baghdad Science Journal
Breast Cancer MRI Classification Based on Fractional Entropy Image Enhancement and Deep Feature Extraction
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Disease diagnosis with computer-aided methods has been extensively studied and applied in diagnosing and monitoring of several chronic diseases. Early detection and risk assessment of breast diseases based on clinical data is helpful for doctors to make early diagnosis and monitor the disease progression. The purpose of this study is to exploit the Convolutional Neural Network (CNN) in discriminating breast MRI scans into pathological and healthy. In this study, a fully automated and efficient deep features extraction algorithm that exploits the spatial information obtained from both T2W-TSE and STIR MRI sequences to discriminate between pathological and healthy breast MRI scans. The breast MRI scans are preprocessed prior to the feature

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Determination Oxidant - Antioxidant Enzyme and some Trace Elements in Breast Cancer in Baghdad City
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level of effectiveness of Glutathione - S - Transferees (GST), Glutathione peroxides (GPX),Malondialdehyde (MDA) the product of lipid peroxidation and some trace elements ( zinc,seleinum,iron ,copper ) had been measured in sera of (50) women with breast disease.which had been divided to : Control group (25),The first group (A) benign breast tumors (25),the second group (B) breast cancer (25). The results showed a clear moral high level of Glutathione - S - Transferees (GST), Glutathione peroxidase (GPX) , and Malondialdehyde (MDA) level in breast cancer group while a slight increase were observed in the levels of these enzymes and(MDA) in benign breast group. A significant reduction was evident in the levels of selenium and zinc

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