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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
Sat Aug 22 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Awareness and knowledge of oral cancer among final year undergraduate dental students in Baghdad-Iraq
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Background: The incidence of oral cancers is increasing all over the world. Early detection ofthis important public health matter makes them more amenable to treatment and allows the greatest chance of cure.The aim of this study was to investigate the awareness and knowledge on oral cancer among final -year dental students in Iraq. Materials and methods: Questionnaires were delivered to 160 final–year dental students in the College of Dentistry in Baghdad. The questionnaire focused on the awareness/knowledge of oral cancer, earlyand common clinical signs and symptoms andassociated risk factors. Results: It was found that 87% of students were aware of oral cancer. The followings were recognized as signs and symptoms of oral cancer: persis

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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
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
Sun Aug 28 2016
Journal Name
World Journal Of Pharmacy And Pharmaceutical Sciences
AN INSIGHT ON THE IDENTIFICATION OF CANCER STEM CELLS USING NOVEL IMMUNOLOGICAL AND MOLECULAR STRATEGIES
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Cancer stem cells (CSCs) are defined as a population of cells present in tumours, which can undergo self-renewal and differentiation. Identification and isolation of these CSCs using putative surface markers have been a priority of research in cancer. With this background we selected pancreatic normal and tumor cells for this study and passaged them into animal tissue culture medium. Further staining was done using alkaline phosphatase and heamatoxilin staining. Blue to purple colored zones in undifferentiated pluripotent stem cells and clear coloration in the chromatin material indicated pancreatic cells. Further studies on the cell surface marker CD 44 were done using ELISA. For this, the protein was extracted from cultivated normal and t

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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
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
Sun Sep 05 2010
Journal Name
Baghdad Science Journal
Chemotherapy Effects on the Activities of Some Purine Metabolic Enzymes in Sera of Ovarian Cancer Patients
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Adenosine deaminase (ADA; Ec: 3.5.4.4), 5´- Nucleotidase (5´– NT; Ec: 3.1.3.5), and AMP – amino hydrolase (AMP – deaminase AMPDA; Ec: 3.5.4.6) activities were measured in sera of ovarian cancer patients before surgery, and after chemotherapy. The results indicated that ADA specific activity increased significantly (P<0.05), while 5´-NT and AMPDA specific activity decreased significantly (P<0.05) in ovarian cancer patients before surgery in comparison with those of their corresponding control women and benign tumors groups. When the activities of these enzymes were measured after chemotherapy, a significant decrease (P<0.05) in ADA activity, and a significant increase (P<0.05) in 5´- NT and AMPDA activities w

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
The inhibition effect of crude juice of olive Olea europeae on cancer cell line Rhabdomyosarcoma (RD)
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The inhibition effect of crude juice of green and black olive on cancer cell line (RD) in vitro has been studied by depending on micro titration system . Eleven different concentration starting from (916-960) mg/ml of crude juice respectively ,for three periods of exposure(24-48-72)hours. The resulted showed that the inhibition effect dependent on type of olive fruit juice ,concentration of dose ,time of exposure and the high concentration of both type of olive juice increased the growth of cell line while other concentration caused decrease in different rates ,moreover the black juice was more effective than green and 48 hours' time exposure was the best for inhibition.

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Publication Date
Sun Aug 21 2022
Journal Name
International Journal Of Health Sciences
Effect of x- ray on the treatment of breast cancer combined with amygdalin and doxorubicin separately
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Background: Radiation therapy has the ability to destroy healthy cells in addition to cancer cells in the area being treated. However, when radiation combines with doxorubicin, it becomes more effective on breast cancer treatment. Objective: This study aims to clarify the effect of X-ray from LINAC combined with amygdalin and doxorubicin on breast cancer treatment, and the possibility of using amygdalin with X-ray instead of doxorubicin for the breast cancer treatment. Method: Two cell lines were used in this study, the first one was MCF-7 cell line and second one was WRL- 68 normal cell line. These cells were preserved in liquid nitrogen, prepared, developed and tested in the (place). The effect of three x-ray doses combined with a

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