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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 Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Few New Carrier Polymers Derived from 2-hydrazinylbenzo[d]thiazole
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2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti

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Publication Date
Fri Jul 01 2022
Journal Name
Archives Of Razi Institute
Prognostic Value of Intracellular Transcription of Factors HIF-1α and p53 and Their Relation to Estradiol and TNM Parameters of Breast Cancer Tissues in Women with Invasive Ductal Carcinoma in Thi-Qar Province, Iraq
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Breast cancer is the most common malignancy affecting women's health, with an increasing incidence worldwide. This study aimed to measure the intracellular concentration of the hypoxia-inducible factor 1 α (HIF-1α), tumor suppression protein p53, and estradiol (E2) in tumor tissues of adult females with breast cancer and their relation to tumor grade, tumor size, and lymph node metastases (LNM). The study was conducted on 65 adult female participants with breast mass admitted to the operating theater in Al-Hussein Teaching Hospital and Al-Habboby Teaching Hospital in Nasiriyah, Iraq, from January to November 2021. Fresh breast tumor tissues were collated and homogenized for intracellular biochemical analysis using the enzyme-linked immuno

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Publication Date
Tue Aug 04 2020
Journal Name
Indonesian Journal Of Pharmacy
Design and Synthesis of Novel Derivatives of 4-(6-(4-Substituted Phenyl)-7H-[1,2,4] Triazolo[3,4-b][1,3,4]Thiadiazin-3- yl) Phenol as a Potent Inhibitor of Tubulin with Antitumor Activity
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Publication Date
Thu May 18 2023
Journal Name
Journal Of Engineering
Experimental Investigation for TiO2 nanoparticles as a Lubricant-Additive for a Compressor ofWindow Type Air-Conditioner
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The coefficient of performance of a window type Air-Conditioner system can be improved if a reduction in the work of compressor can be achieved by a suitable technique. The present study investigates the effect of dispersing a low concentration of TiO2 nanoparticles in the mineral oil based lubricant, as well as on the overall performance of a window type Air-Conditioner system using R22 as the working fluid. An enhancement in the COP of the refrigeration system has been observed and the existence of an optimum volume fraction noticed, with low concentrations of nanoparticles suspended in the mineral oil. Results showed that the average compressor work reduced by 13.3%, which ultimately resulted in an increase of 11.99% in the COP due to

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Publication Date
Sat Mar 25 2017
Journal Name
Biomedical And Pharmacology Journal
Detection of Cytomegalovirus and Epstein Barr Virus in Placental Tissues of Aborted Women
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Introduction The abortions reasons in several circumstances yet are mysterious, nevertheless the bacterial toxicities signify a main reason in abortion, where germs seems to be the utmost elaborate pathogens (Khameneh et.al., 2014) and (Oliver and Overton ,2014). Between numerous germs, Humano

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Publication Date
Sat Jun 30 2012
Journal Name
Al-kindy College Medical Journal
Correlation of Concentrations of Certain Trace Elements in Normal and Diseased Human Tissues
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Background Over the past decade there has been a growing awareness of, and interest in, the trace element concentration differences between normal and diseased tissues. Significant changes in tissue concentrations of Zinc (Zn) and Copper (Cu) have been previously reported in inflammation and cancer of certain human tissues.
Aim:(1)To correlate between Zn and Cu concentrations and the histological picture of normal and certain inflamed human tissues, namely the gall bladder (GB) the vermiform appendix (VA), visceral adipose tissue (VAT) and subcutaneous adipose tissue (SAT). (2) to detect whether there is a difference in the above-mentioned parameters between VAT and SAT. (3) to obtain recordings for trace element levels in human tissu

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Publication Date
Thu Nov 01 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Quality of Life Assessment for Patients with Colorectal Cancer
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Abstract A descriptive study to assess the quality of life (QOL) for patients with colorectal cancer. The study was conducted from Baghdad Teaching Hospital, Al-Yarmouk Teaching Hospital and Radiation Hospital and Nuclear medicine for the period from 1st July/2004 to 1st September/2004. The sample selected by purposive random of (50) patients diagnosed with colorectal cancer and all of them who were under chemotherapy treatment. A questionnaire was prepared for the purpose of the study and comprised of three parts including: 1- Socio-demographical characteristics. 2- Clinical characteristics. 3- and QOL

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Publication Date
Sun Dec 09 2018
Journal Name
Baghdad Science Journal
Detection of Pseudomonas aeruginosa in Clinical Samples Using PCR Targeting ETA and gyrB Genes
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Pseudomonas aeruginosa has variety of virulence factors that contribute to its pathogenicity. Therefore, rapid detection with high accuracy and specificity is very important in the control of this pathogenic bacterium. To evaluate the accuracy and specificity of Polymerase Chain Reaction (PCR) assay, ETA and gyrB genes were targeted to detect pathogenic strains of P. aeruginosa. Seventy swab samples were taken from patients with infected wounds and burns in two hospitals in Erbil and Koya cities in Iraq. The isolates were traditionally identified using phenotypic methods, and DNA was extracted from the positive samples, to apply PCR using the species specific primers targeting ETA, the gene encoding for exotoxin A, and gyrB gene. The res

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Publication Date
Thu Mar 05 2020
Journal Name
Revista Brasileira De Farmacognosia
Zerumbone-Loaded Nanostructured Lipid Carrier Gel Facilitates Wound Healing in Rats
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Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
CA 27-29: A Valuable Marker for Breast Cancer Management in Correlation with CA 15-3
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