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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
Sun Sep 15 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Novel Candidate Single Nucleotide Polymorphisms of ERCC2 Gene that Influence Colorectal Cancer Susceptibility
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Colorectal cancer (CRC) is the most common gastrointestinal malignancy and one of the top ten common cancers worldwide with approximately 2 million cases. There are multiple risk factors that could lead to CRC emergence; of which are genetic polymorphisms. Excision repair cross-complementing group 2 (ERCC2) gene encodes for ERCC2 enzyme which plays a crucial role in maintaining genomic integrity by removing DNA adducts. Several studies suggested that there could be a link between genetic polymorphisms of ERCC2 gene and the risk of CRC development. Hence the present study aims to validate the relationship between the following ERCC2 single nucleotide polymorphisms (rs13181, rs149943175, rs530662943, and rs1799790) and CRC susceptibility. A t

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Publication Date
Mon Jun 01 2020
Journal Name
P J M H S
The influence of Breast Cancer Molecular Subtypes on Metastatic pattern in Iraqi patients
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Publication Date
Fri Jul 12 2019
Journal Name
International Journal Of Research In Pharmaceutical Sciences
Uranium concentration variation dependency on gender correlated with age of bladder cancer patient
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Human health was and still the most important problem and objective of all most researches. Finding out what causes in the decadence of healthiness of Iraqi population is our tendency in the present work, Uranium causing cancer that is affected by a correlation between age and gender of bladder cancer patients is studied in the present work. Mean of Uranium concentration (Uc) decreased with increasing age for all age group without dependency on gender. While, there is a wide dispersion in Mean Uc excretion between males and females, due to the effect of correlated gender with age, where female Mean Uc is maximum at age 50-69 year (2.355 µg/L), and it's higher than male Mean Uc (2.022 µg/L) in this age stage because of menopause, a

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Publication Date
Thu Jun 30 2011
Journal Name
Al-kindy College Medical Journal
The Expression of Epstein-Barr virus in Breast cancer in relation to age
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Background: Breast cancer is the most common
malignancy affecting females worldwide. The association
of Epstein-Barr virus (EBV) with this cancer is a longstanding
interest to this field.
Aim: to investigate the presence of EBV in breast tumor
tissue in relation to age.
Patients and Methods: Paraffin-embedded tissue blocks
from 45 female patients with breast tumors (ranged in age
from 28 to 85 years) were retrieved. The cases were
grouped into two categories: group (A): included 30 cases
with breast carcinoma and group (B): included 15 cases
with benign breast diseases as a control group .The
expression of EBV protein was examined
immunohistochemically.
Results: Twelve (40%) of the 30 breast canc

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Publication Date
Mon Jan 01 2018
Journal Name
Indian Journal Of Public Health Research & Development
Immunohistochemical Expression of CDX2 Protein in Iraqi Patients with Human Gastric Cancer (HGC)
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This study aimed to evaluate the IHC expression of CDX2 protein in HGC patients and control groups and also to study the correlation between IHC expression of the CDX2 and different clinicopathological variables such as: age, gender, histopathological subtype, grade, and stage of the tumor in HGC cases. the retrospectively sectional study for the period from 2014 to 2018 included a total of 60 formalin fixed paraffin embedded blocks of the HGC tissue (partial or total gastrectomy specimens) that collected from the archived materials of the Department of Pathology of Baghdad Teaching Hospital and the Center of Gastrointestinal and Hepatic Diseases, and also some samples were collected from other private laboratories. The IHC expression of th

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Publication Date
Thu Jun 08 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Detection of BRAF Gene in Some Iraqi Bowel Inflammation and Colorectal Cancer Patients
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The impacts of the inflammatory process on neoplasia development were observed in many cancer, it has a great role in the etiology, development and progression of invasive colorectal tumors. This study was designed to investigate the BRAF mutation and assist the clinicopathological parameter in some Iraqi bowel inflammation and colorectal cancer patients. Thirty patients were enrolled in this study (15 suffering bowel inflammation and 15 having colorectal cancer). BRAF gene was screened for the presence of mutations using PCR technique and direct  sequencing. .The results revealed no BRAF mutation in position 1799 for exon fifteen in both samples of bowel inflammation and colorectal cancer. These results were confirmed previous arti

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Publication Date
Thu Jan 07 2016
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Determination of Some Trace Element Levels in Iraqi Male patients with Colorectal Cancer
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Alterations of trace element concentrations adversely affect biological processes and could promote carcinogenesis. Trace element deficiency or excess is implicated in the development or progression of some cancers like colorectal cancer. The aim of the present study was to compare the serum copper (Cu) and zinc (Zn) concentrations in patients with colorectal cancer from Iraqi male patient with those of healthy subjects. During the period of March 2015 until august 2015, a total of 25 patients with metastatic colon cancer and 20 healthy volunteers were enrolled from the Al-Kadhimia Teaching Hospital after the diagnosis using a histopathological examination for the malignant tumor; their age was between (38-60) years. Higher levels o

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Publication Date
Sat Mar 11 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Determination of Some Trace Element Levels in Iraqi Male patients with Colorectal Cancer
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   Alterations of trace element concentrations adversely affect biological processes and could promote carcinogenesis. Trace element deficiency or excess is implicated in the development or progression of some cancers like colorectal cancer. The aim of the present study was to compare the serum copper (Cu) and zinc (Zn) concentrations in patients with colorectal cancer from Iraqi male patient with those of healthy subjects. During the period of March 2015 until august 2015, a total of 25 patients with metastatic colon cancer and 20 healthy volunteers were enrolled from the Al-Kadhimia Teaching Hospital after the diagnosis using a histopathological examination for the malignant tumor; their age was between (38-60) years. Higher

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Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Assessment of Some Hematological parameters in Iraqi Women with Different Breast Cancer Stages
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Breast cancer (BC) is the most commonly diagnosed cancer in women. The metabolism of iron is closely regulated by hepcidin which exerts its action by interacting with a ferroportin.

 The aim of the present study was to assess the alterations in the levels of some serum biomarkers that have a role in iron homeostasis (hepcidin and ferroportin) in addition to hematological parameters (hemoglobin, leukocyte and platelets count) in different stages of BC.

This study included 66 women with BC. The patients were categorized as follows : group 1 includes :22 patients with stage I disease ,group 2 includes: 22 patients with stage II disease ,and group 3 include: 22 patients with stage III disease .Group 4 includes :22 appare

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Publication Date
Tue Feb 26 2019
Journal Name
Journal Of Contemporary Medical Sciences
Demographic and clinical profiles of female patients diagnosed with breast cancer in Iraq
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Objective To highlight the main demographic characteristics and clinical profiles of female patients registered with breast cancer in Iraq; focusing on the impact of age.Methods This retrospective study enrolled 1172 female patients who were diagnosed with breast cancer at the Main Center for Early Detection of Breast Cancer/Medical City Teaching Hospital in Baghdad. Data were extracted from an established information system, developed by the principal author under supervision of WHO, that was based on valid clinical records of Iraqi patients affected by breast cancer. The recorded information regarding clinical examination comprised positive palpable lumps, bloody nipple discharge, skin changes, bilateral breast involvement, tumor

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