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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 28 2025
Journal Name
Polymers
Characterization of a Hydrogel Composite Containing Bioactive Moringa as a Novel Pulp-Capping Material
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Hydrogels are hydrophilic biocompatible polymers that can be used as a drug delivery material in different medical branches, including vital pulp therapy. The aim of this study is to characterize the physical and biological properties of the newly developed formula as a candidate direct pulp-capping material. The hydrogel composite was prepared from natural and synthetic origins (polyvinyl alcohol (PVA), hyaluronic acid (HA), and sodium alginate (SA)) with the incorporation of bioactive Moringa. Different formulas of hydrogel containing different concentrations were evaluated for physicochemical (FTIR, XRD, SEM, degradation, and swelling), mechanical (viscosity, folding endurance, film thickness), and biological (antioxidant, antibacterial,

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Publication Date
Wed Apr 30 2014
Journal Name
Oncotarget
‘Sex’ in the cancer cell
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The development of better tools for diagnosis and more accurate prognosis of cancer includes the search for biomarkers; molecules whose presence, absence or change in quantity or structure is associated with a particular tumour or prognosis/therapeutic outcome. While biomarkers need not be functionally relevant, if cell survival, then they could also provide new targets for therapeutic drugs. In recent years attention has been applied to a group of proteins known as cancer testis antigens (CT antigens) [1]. These proteins are products of genes whose expression was normally confined to the testis, yet they are expressed in tumour cells. CT genes are bound to serve a wide array of roles in the testes, which have many highly differentiated cel

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Publication Date
Thu Jan 07 2021
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Review: Cancer Cells Resistance Strategies
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Publication Date
Tue Jan 29 2019
Journal Name
Frontiers In Cell And Developmental Biology
Hypoxia-Modified Cancer Cell Metabolism
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Publication Date
Fri Nov 09 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Psychological Problems of Patients with Colorectal Cancer
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Objective: Assessment the psychological problems in patients with colorectal cancer, and to find out the
relationship between socio-demographic characteristics such as (age, sex, marital status, educational level,
and occupation) and psychological problems for those patients.
Methodology: A descriptive design is employed through the present study from 1
st July 2011 to 25
th December
2011 in order to study the quality of life in colorectal cancer patients with psychological problems.
A purposive (non probability) sample is selected for the study which includes (60) patients diagnosed with
colorectal cancer were treated in Mosul Oncology and Nuclear Medicine hospital or the patients who visited
the outpatient cl

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Publication Date
Sat Dec 30 2023
Journal Name
Wasit Journal For Pure Sciences
A Review of Modern Methods of Synthesis 1, 3, 4-Oxadiazole as a Bioactive Compounds
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ABSTRACT: Oxadiazole ring is a heterocyclic molecule with an oxygen and two nitrogen atoms spread throughout its five-membered structure. There are four different isomers that have been discovered, Because of their wide applications in a range of sectors, including medications . Some of these biological activity are; anticonvulsant capacity, anticancer as well, antibacterial, antiviral, antifungal,  antimalarial, antitubercular, anti-asthmatic, antidepressant, antidiabetic, antioxidant, antiparkinsonian, analgesic and  anti-inflammatory, are just some of the therapeutic uses that have drawn attention to drug candidates containing an oxadiazole moiety. This review, we will examine the various methods of oxadiazole synthesis. The mo

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Publication Date
Wed Aug 30 2023
Journal Name
Baghdad Science Journal
The Influence of Obesity and IL-6 on Infertile Iraqi Women with COVID-19 Complications
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Infertility is one of the types of diseases that occur in the reproductive system. Obesity is a state that can be occurred due to excessive fats, the progression in obesity stage results in a change in adipose tissue and the development of chronic inflammation, endocrine glands disorders and women’s reproductive system, and also increase the infection with covid-19. The study aimed to investigate the effect of the obesity, lipid-profile, and IL-6 on hormones-dysregulation in infertile-women with COVID-19 complications. The current study included 70 samples: 50 infertility-women-with-covid-19-infected, 20 healthy-women/control, the ages of both patients and healthy subjects were selected within the range 18-34 years. Levels of FBS, LH,

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Publication Date
Sun Sep 05 2010
Journal Name
Baghdad Science Journal
Detection of interleukin-6 and interleukin-8 in serum from women with recurrent spontaneous abortion
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To investigate the role of IL-6 and IL-8 in the immune-regulatory mechanisms involved in the recurrent spontaneous abortion of the first trimester of pregnancy. Serum level of IL-6 and IL-8 were determined in 25 women of age (20-35) years who had a spontaneous abortion of unknown aetiology during the first trimester of pregnancy .They were compared with the corresponding levels of 20 pregnant and non-pregnant women as control groups .cytokine levels were measured by (ELISA) technique .The women with spontaneous abortion had highly significant (P < 0.01) increased serum level of IL-8 and highly significant (P < 0.01 ) decreased level of IL-6 compared to those with normal pregnant and non-pregnant women. The results of this study ma

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Publication Date
Mon Apr 01 2019
Journal Name
Indian Journal Of Public Health Research And Development
Analysis of Serum Il-6 and CRP Levels among Autoimmune and Non- Autoimmune Hypothyroid Patients
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Hashimoto Thyroiditis (HT) is the most common autoimmune thyroid disease and the commonest cause ofhypothyroidism. C-reactive protein (CRP) is synthesized in hepatocyte in response to autoimmune disorders;strongly induced by IL-6. This study aimed to estimate serum IL-6 and CRP levels in autoimmune and non-autoimmune hypothyroidism. The present study included 60 Iraqi female hypothyroid patients divided to 30autoimmune and 30 non-autoimmune, with age ranged between 24-50 years and 30 healthy controls withage ranged between 27-52 years. Serum samples were collected from study groups. The levels of thyroidhormones (TSH, T4 and T3) were determined by using automated Chemiluminescence Immunoassay (CLIA)analysis system. Detection the levels of t

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Publication Date
Sun Oct 31 2021
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn: 2789-3219 )
Evaluation of EOS Gene Expression and IL-6 Serum Levels in Iraqi Patients with Psoriasis
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Background: EOS (encoded by the IKZF4 gene) is a member of the zinc finger transcription factor IKaros family, and plays a critical role in Treg suppressor functions, and maintaining Treg stability. IL-6 is a soluble mediator with a pleiotropic effect on inflammation, immune response, and hematopoiesis. Aim: To estimate serum IL-6 level and EOS gene expression in Iraqi patients with psoriasis. Method: Twenty-two patients with psoriasis (8 females, 14 males) with age ranged 18-72 years, were recruited from Baghdad Teaching Hospital, Dermatology Clinic, Baghdad, and 24 healthy donors. The serum levels of IL-6 by ELISA and the gene expression of IKZF4 (EOS gene) by RT-qPCR technique. Results: The results showed a non-significant diffe

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