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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
Thu Jan 01 2015
Journal Name
International Journal Of Technical Research And Applications
SYNTHESIS OF DRUG CARRIER POLYACRYLIC ACID WITH SPACER GROUP
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Publication Date
Tue May 01 2018
Journal Name
Journal Of Information Engineering And Applications
Development of Prognosis Factors in a Scoring System for Predicting of Breast Cancer Mortality
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Today, the prediction system and survival rate became an important request. A previous paper constructed a scoring system to predict breast cancer mortality at 5 to 10 years by using age, personal history of breast cancer, grade, TNM stage and multicentricity as prognostic factors in Spain population. This paper highlights the improvement of survival prediction by using fuzzy logic, through upgrading the scoring system to make it more accurate and efficient in cases of unknown factors, age groups, and in the way of how to calculate the final score. By using Matlab as a simulator, the result shows a wide variation in the possibility of values for calculating the risk percentage instead of only 16. Additionally, the accuracy will be calculate

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Publication Date
Fri Jul 24 2020
Journal Name
Al-kindy College Medical Journal
A review study of targeting of AAK1 and JAK1/2 using baricitinib in COVID-19 infected human cells
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     The outbreak of a current public health coronavirus 2019 disease is a causative agent of a serious acute respiratory syndrome and even death. COVID-19 has exposed to multi-suggested pharmaceutical agents to control this global disease. Baricitinib, a well-known antirheumatic agent, was one of them. This article reviews the likely pros and cons of baricitinib in attenuation of COVID-19 based on the mechanism of drug action as well as its pharmacokinetics. The inhibitory effect of baricitinib on receptor mediated endocytosis promoter, AKK1, and on JAK-STAT signaling pathway is benefacial in inhibition of both viral assembling and inflammation. Also, its pharmacokinetic has encouraged the physicians toward the drug

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Publication Date
Sun Jun 30 2024
Journal Name
Romanian Medical Journal
Serum and urine apolipoprotien A1 (ApoA1) as biomarkers in bladder cancer
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Bladder cancer (BC) is the predominant malignant neoplasm in the urinary system and ranks as the tenth most prevalent malignant tumor worldwide. Compared with females, males displayed a four-fold more common incidence of bladder cancer. It mainly affects men. Bladder cancer is the fourth most prevalent neoplasm in males. The most important protein that makes up high density lipoprotein (HDL), ApoA-I apolipoprotein A1 is essential in regulating the right amount of cholesterol. Multiple inquiries have demonstrated that APOA1 plays a pivotal role in the progression, infiltration, and spread of tumors. Objectives. The objective of this study was to measure the level of urine to serum apolipoprotein A1 in patients suffering from bladder

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Publication Date
Mon Jan 01 2024
Journal Name
Oncology And Radiotherapy
Comparting study of cytokeratin 18 fragment M65 with CA19-9 and CEA as a biomarker in Iraqi colon cancer patients
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Publication Date
Fri Sep 26 2025
Journal Name
Iraqi Journal Of Embryos And Infertility Researches
Study of Interleukin-6 (IL-6) Profile in the Seminal Fluid of Oligozoospermia Men
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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Osteocalcin as a Biomarker for Estimation of Infertility for Iraqi Patients
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Objective: The evaluation of serum osteocalcin (OSN) for Iraqi infertile patients to see the effect of osteocalcin insufficiency, which may lead to a decreased level of testosterone production in males that may cause infertility. Methods: Forty two newly diagnosed infertile males age range (24–47) years and thirty two apparently healthy males as controls age range (25–58) years. Serum levels of testosterone (TEST), stimulating follicle hormone (FSH) and luteinizing hormone (LH), prolactin (PROL), osteocalcin OSN, and fasting blood sugar (FBS) were performed in both patients and controls. Estimation of serum OSN by Immulite1000 auto-analyzer, TEST, FSH, LH, PROL, and FBS by Immulite2000 auto-analyzer. Results: Infertile patients

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Publication Date
Sun Sep 26 2021
Journal Name
Modern Sport
Effect of Rehabilitation Program by Using Hypermedia on Treatment Some of Shoulder Tissues Injuries for Badminton Players
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The important of present study is to design rehabilitation program by using hypermedia for some injuries of smooth tissues in shoulder joint.   This joint is most important to help badminton players in achieving their daily and sport tasks due to upper limp movements depend on health and active of this joint. Experimental approach with a manner of equal single station was used in present study and study simple consisted of 6 badminton players from Babylon and Al-Mahaweel clubs who have less sharp tissue smooth injury such (muscles, ligaments, pocket). We used (SPSS) to analyses pre, medal, post-tests data. In conclusion, hypermedia is positive benefit to rehabilitee of injuries of smooth tissues in shoulder joint for badminton pla

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Publication Date
Fri Jan 01 2010
Journal Name
International Journal Of Communication Networks And Distributed Systems
A novel Radon-based multi-carrier direct sequence code division multiple access transceiver design and simulation
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Multi-carrier direct sequence code division multiple access (MC-DS-CDMA) has emerged recently as a promising candidate for the next generation broadband mobile networks. Multipath fading channels have a severe effect on the performance of wireless communication systems even those systems that exhibit efficient bandwidth, like orthogonal frequency division multiplexing (OFDM) and MC-DS-CDMA; there is always a need for developments in the realisation of these systems as well as efficient channel estimation and equalisation methods to enable these systems to reach their maximum performance. A novel MC-DS-CDMA transceiver based on the Radon-based OFDM, which was recently proposed as a new technique in the realisation of OFDM systems, will be us

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Publication Date
Wed Aug 31 2022
Journal Name
Al-kindy College Medical Journal
Left Flank Pain and Hydronephrosis as the Initial Presentations of Advanced Gastric Cancer
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Ureteric obstruction is rarely noted in cases of gastric cancer. Its involvement by distant metastasis from gastric adenocarcinoma without direct invasion is an exceptionally unusual occurrence. This is the story of a 58-year-old man who arrived at the emergency department with acute flank pain and fever. He was initially diagnosed with obstructive pyelonephritis after the discovery of a new onset, complete ureteric obstruction on the left side. Subsequent investigations and follow-up revealed the presence of gastric adenocarcinoma with possible ureteric metastasis bilaterally, flank pain and hydronephrosis were the first and only presentations of gastric cancer. The rarity of the condition and the unusual presentation encouraged us to r

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