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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
Fri Mar 14 2025
Journal Name
Obat: Jurnal Riset Ilmu Farmasi Dan Kesehatan
Chemical Productions and Immunological Assessments of Cancer Vaccines According to Α-Galactosylceramide and Ganglioside Antigen
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iNKT cells, sometimes known as the immune system's "Swiss Army knife," have become key components of cancer vaccination treatments. Glycolipids that activate iNKT cells, including α-galactosylceramide (αGalCer), have been used to create self-adjuvanting anti-tumor vaccinations and can boost the immune response to co-delivered cancer antigens. The chemicals synthesis of ganglioside antigens, specifically (Neu5Gc) GM3 and GM3 antigen, and conjugations to αGalCer, and packaging into liposome as effective platforms for their in vivo deliverying are the main topics of this work. In mouse and human cell experiments, liposome containing, (Neu5Gc) GM3-αGalCer, GM3-αGalCer, and equimolar quantities of conjugates have thoroughly describe

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Publication Date
Fri Jan 31 2025
Journal Name
Aip Conference Proceedings
Classification of oral cavity cancer using linear discriminant analysis (LDA) and principal component analysis (PCA)
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Publication Date
Tue May 01 2012
Journal Name
Iraqi Journal Of Physics
Early detection of breast cancer mass lesions by mammogram segmentation images based on texture features
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Mammography is at present one of the available method for early detection of masses or abnormalities which is related to breast cancer. The most common abnormalities that may indicate breast cancer are masses and calcifications. The challenge lies in early and accurate detection to overcome the development of breast cancer that affects more and more women throughout the world. Breast cancer is diagnosed at advanced stages with the help of the digital mammogram images. Masses appear in a mammogram as fine, granular clusters, which are often difficult to identify in a raw mammogram. The incidence of breast cancer in women has increased significantly in recent years.
This paper proposes a computer aided diagnostic system for the extracti

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Publication Date
Sun Dec 09 2018
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Poly Heterocyclic Compounds, and Effect on Cancer Cell (Hep-2) In vitro.
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A synthesis series of new heterocyclic derivatives (A2-A7) (pyrrole, pyridazine, oxazine and imidazol) derived from 4-acetyl-2,5-dichloro-1-(3,5-dinitrophenyl)-1H-pyrrole-3-carboxylate(A1) have been synthesised. Synthesis of compound (A2) by the reaction of starting material (A1) with hydroxyl amine hydrochloride in the presence of pyridine. Compound (A2) was reacted with hydrazine hydrate in dry benzene to give (A3) derivative. The compound )A3( deals with sodium nitrite to give diazonium salt, and the reaction diazonium salt with ethyl acetoacetate to produce compound (A4). To a mixture of compound (A4) and hydroxyl amine with sttired to yield (A5).Compound (A6) was prepared by reaction compound (A4) with thiosemicarbazide in presence

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Publication Date
Thu Aug 13 2020
Journal Name
Asia Pacific Journal Of Molecular Biology And Biotechnology
The anticancer molecular mechanism of Carnosol in human cervical cancer cells: An in vitro study
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Carnosol, a phenolic diterpene, is one of the effective anticancer agents naturally occurring in rosemary, sage, parsley, and oregano. The chemoresistance problem increased with the routinely used chemotherapy. Therefore, the efforts to find a substitute with safe and low cost have become crucial worldwide. The current study attempts to inspect the anticancer molecular mechanisms of Carnosol on modulating up- and down- regulation of multiple genetic carcinogenesis pathways. The cytotoxicity of Carnosol on Hela cells was evaluated by MTS assay. Flow cytometry was used to assess apoptosis and cell cycle arrest. The apoptotic morphological changes were obvious by dual apoptosis assay. The differential gene expression after treatment wi

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Publication Date
Sat May 01 2021
Journal Name
Journal Of Physics: Conference Series
Antioxidant, cytotoxicity and phytochemical analysis of Larinus maculates F. cocoon aqueous extract against lung cancer
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Abstract<p>Cocoon of larva <italic>Larinus maculates</italic> F. from Curculionidae family (<italic>Echinops</italic> species), locally in Iraq known as Tihan, is one of traditional folk medicine used in the treatment of diversity respiratory system and fever. This study was carried out to assess the bioactive component and the antioxidant capability of aqueous beetle cocoon extract (<italic>Larinus maculates</italic> F.) along with its possible cytotoxic activity against A549 lung cancer cell line. For phytochemical analysis gas chromatography-mass spectrometry (GC-MS) was used, and to detected free scavenging activity 2, 2-diphenyl-1 picrylhydrazyl (DPPH) was used</p> ... Show More
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Publication Date
Mon Apr 01 2024
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Impact of Clinical Pharmacist Intervention on Chemotherapy Knowledge, Attitude, and Practice among Breast Cancer Women
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الخلفية: إن سمية الدواء والآثار الجانبية للعلاج الكيميائي تؤثر سلبا على مرضى سرطان الثدي. الأهداف: لتقييم فعالية التدخلات الصيدلانية في تحسين معرفة مرضى سرطان الثدي ومواقفهم وممارساتهم فيما يتعلق بالعلاج الكيميائي لسرطان الثدي.

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Publication Date
Fri Jun 07 2024
Journal Name
Asian Pacific Journal Of Cancer Prevention
The Effect of NF-κB Deactivation on Cancer Cell Response to ALA Mediated Photodynamic Therapy
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due to the presence of chemoresistance and the risk of tumor recurrence and metastasis. There is a pressing necessity to develop efficient treatments to improve response for treatment and increase prolong survival of breast cancer patients. Photodynamic therapy (PDT) has attracted interest for its features as a noninvasive and relatively selective cancer treatment. This method relies on light-activated photosensitizers that, upon absorbing light, generate reactive oxygen species (ROS) with powerful cell-killing outcomes. Nuclear factor kappa B (NF-κB), a transcription factor, plays a key role in cancer development by regulating cell proliferation, differentiation, and survival. Inhibiting NF-κB can sensitize tumor cells to chemotherapeuti

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Publication Date
Sun Jun 01 2014
Journal Name
Alustath Journal For Human And Social Sciences
Obstacles to the application of electronic management in university libraries: the universities of Baghdad and Al-Mustansiriya as a model.
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The research aims to identify the obstacles facing the application of electronic management in our university libraries, including the central library of the University of Baghdad and the central library of Al-Mustansiriya University, the research sample, as they are among the main libraries that used electronic technologies in managing some of their work and in providing their services, and they have a website via the Internet. The research relied on the case study method to identify the obstacles by visiting the two libraries, interviewing their managers and employees responsible for the departments, and answering inquiries about the obstacles that prevent the application of electronic management in order to identify them and find appropr

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Publication Date
Thu Oct 01 2015
Journal Name
Journal Of Educational And Psychological Researches
Anxiety of death among pregnant women in the light of some Demographic variables Governorates Bethlehem and Tulkarm as a model
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This study aims to identify the anxiety pregnant women have of dying, in the light of some Demographic variables in Bethlehem (age, residence, and the mother's job). The descriptive method was used in this study. To achieve the study purposes, the researchers developed a questionnaire as a tool of study, which consisted of (19) paragraphs ,after been verified of its validity & stability.

The researchers distributed questionnaires, and then analyzed them. Results illustrated that the levels of anxiety pregnant women in Bethlehem had of dying was average,  with a mean total score of (3.11),  and with a standard deviation that had the total score of (0.476). Results also illustrated statistical differences in the pregn

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