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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
Thu Jan 23 2025
Journal Name
Научный форум
PHRASEOLOGISMS RELATED TO THE USE OF COLORS IN SPEECH AS A MEANS OF ENRICHING MODERN RUSSIAN LANGUAGE
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The paper examines key aspects of the use of phraseologi-cal units related to colors in Russian culture and speech. It explores their role in shaping cultural identity, reflecting national characteristics and men-tality. The study analyzes the frequency and contexts of the use of color-related phraseological units in contemporary speech, as well as the influ-ence of media and literature on their popularization. The author highlights the significance of phraseological units in preserving cultural heritage and fostering a deeper understanding of language and culture.

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Publication Date
Wed Aug 30 2023
Journal Name
Baghdad Science Journal
Impact of COVID-19 Vaccine on Hearing Status of Young Ages (Medical College Students as a Sample)
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Many studies dealt with the consequences of  SARS CoV-2  (which cause COVID-19 infection) on the nervous system especially sensory nerves where the virus causes loss of taste and smell as it’s known, and may affect auditory nerves and be the expected cause of some hearing problems. A case-control analytic study was performed on a connivance sample of society of university students from a medical faculty. Each participant filled out a questionnaire contains demographic data and general, auditory and respiratory health condition, in addition to vaccination status. In the other side, the audio- examinations were performed on the study sample including Pure Tone Audiometry (PTA) and tympanometry. Two statistical methods; chi-square and t

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Publication Date
Fri Feb 28 2020
Journal Name
Neuroquantology
Using X-Ray Films for Evaluation efficiency of Unsaturated Polyester Reinforced by Lead Oxide as Shielding for Medical X-ray Devices
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The largest use of x-ray in medical by dentists, employers or persons that needed by patients with specific conditions, lead to higher exposure of x-ray that may cause many diseases. In the present work radiography films have been used in evaluating the efficiency of using unsaturated polyester polymer reinforced with lead oxide (PbO) as shield material for medical x-ray devices, many parameters studied like concentration and thickness that they are increasing the attenuation of x-ray in them. The results show that the attenuation of X-ray increasing with concentration of reinforced material and with thickness, and the optical density decreases with increasing concentration from 0% to 50%, we chose 30% as suitable concentration to increase

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Publication Date
Thu Dec 31 2020
Journal Name
Political Sciences Journal
Russian-American competition in the Middle East:Power and roles conflict: Syria as a model
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Because of its importance in the world, Middle East area is one of the competition areas between the major and great powers. Among those powers are Russia and United states of America. The competition between these two powers to control Syria is greatly clear since 2011. It is also one of the most important subject in the international politics. This importance comes from the importance of Russia and the United States of America besides importance of the Middle East. At the end of the cold war, United States of America maintained its role in the international system and became the only pole that dominated the international affairs while Russia tried to overcome the challenges inherited from the former Soviet Union, and it succeeded in th

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Publication Date
Tue Oct 01 2019
Journal Name
2019 12th International Conference On Developments In Esystems Engineering (dese)
Roadway Deterioration Prediction Using Markov Chain Modeling (Wasit Governorate/ Iraq as a Case Study)
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Publication Date
Fri Mar 01 2024
Journal Name
Annales Pharmaceutiques Françaises
Adopting video assignments as a tool to improve first-year pharmacy students class engagement
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Publication Date
Sun Oct 01 2023
Journal Name
Minerva Dental And Oral Science
Salivary interleukin-1β as a biomarker to differentiate between periodontal health, gingivitis, and periodontitis
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Publication Date
Sun Mar 25 2018
Journal Name
Biomedical And Pharmacology Journal
Anti CD20 Monoclonal Antibody (Rituximab) as a Rescue Treatment in Severe and Refractory SLE
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Systemic lupus erythematosus (SLE) is an autoimmune disease with polymorphic expression. B cells have an essential contribution in immune system activation via the production of different cytokines and functioning as potent antigen-presenting cells. Therefore, a drug that particularly targets B cells may represent an ideal therapeutic approach for SLE. Rituximab (RTX), an anti-CD20 monoclonal antibody causing transient B-cell depletion, has been used to manage SLE. This study aims to assess Rituximab effects on lupus nephritis (LN) patients when added to conventional immunosuppressants. Twenty four patients, 15-32 years old, with class III/IV/V LN were involved in this study. All were on steroids before lupus nephritis occurrence. They were

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Publication Date
Wed May 10 2017
Journal Name
Journal Of The College Of Languages (jcl)
Technical methods in foreign language teaching as a new method in foreign language learning
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Unter dem Titel " Technische Methoden im Fremdsprachunterricht als eine neueste Methode im Fremdsprachlernen, die Spiele als Muster"

versteht man, dass die Forschung  sich mit einer neuen Methoden im Fremdsprachunterricht beschäftigt. Von den neuen Methoden im Unterricht sind die Spiele. So man sieht  in den letzten Jahren viele Artikel zum Thema Spiele im Fremdsprschunterricht. Davon gehen wir aus, dass die Spiele im Unterricht eine groβe Rolle spielt, denn diese Methode macht Lust, Spaβ im Lernenprozeβ. Die Spiele im Unterricht bezeichnen als ein Mittel, um Unterricht etwas Schönes , Nützliches und Lebendigs zu sein. Die Spiele sind vielfälltig und unterscheidet sich nach den Themen und Materialien. In dieser F

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Publication Date
Sun Mar 25 2018
Journal Name
Biomedical And Pharmacology Journal
Anti CD20 Monoclonal Antibody (Rituximab) as a Rescue Treatment in Severe and Refractory SLE
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Systemic lupus erythematosus (SLE) is an autoimmune disease with polymorphic expression. B cells have an essential contribution in immune system activation via the production of different cytokines and functioning as potent antigen-presenting cells. Therefore, a drug that particularly targets B cells may represent an ideal therapeutic approach for SLE. Rituximab (RTX), an anti-CD20 monoclonal antibody causing transient B-cell depletion, has been used to manage SLE. This study aims to assess Rituximab effects on lupus nephritis (LN) patients when added to conventional immunosuppressants. Twenty four patients, 15-32 years old, with class III/IV/V LN were involved in this study. All were on steroids before lupus nephritis occurrence. They were

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