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bijps-563
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
Wed Jan 01 2020
Journal Name
Desalination And Water Treatment
Combination of the artificial neural network and advection-dispersion equation for modeling of methylene blue dye removal from aqueous solution using olive stones as reactive bed
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Publication Date
Tue Dec 07 2021
Design and numerical verification of a polarization-independent grating coupler using a double-layer approach for visible wavelengths applications
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Publication Date
Wed Jan 01 2014
Journal Name
Scienceasia
A combined compact genetic algorithm and local search method for optimizing the ARMA(1,1) model of a likelihood estimator
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In this paper, a compact genetic algorithm (CGA) is enhanced by integrating its selection strategy with a steepest descent algorithm (SDA) as a local search method to give I-CGA-SDA. This system is an attempt to avoid the large CPU time and computational complexity of the standard genetic algorithm. Here, CGA dramatically reduces the number of bits required to store the population and has a faster convergence. Consequently, this integrated system is used to optimize the maximum likelihood function lnL(φ1, θ1) of the mixed model. Simulation results based on MSE were compared with those obtained from the SDA and showed that the hybrid genetic algorithm (HGA) and I-CGA-SDA can give a good estimator of (φ1, θ1) for the ARMA(1,1) model. Anot

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Publication Date
Mon May 27 2019
Journal Name
Al-academy
A Hypothesis of Architectural Environment Exercise for Actor Training (Continuous exercise space workshop – A model): هيثم عبد الرزاق علي
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The peculiarity of the theater does not lie in its dramatic content because many literary genres and other artistic styles share with it in this content. The peculiarity of the theater lies in contemplating the drama through what is architectural, and this architectural axis is what distinguishes its character. It is a spatial poetry which is composed by the laws of physics and chemistry, (Weight, height, distance, rhythm, gravity, impulses and chemical excretions). i.e., what cannot be expressed in words. This is a game of space to exchange and organize energy and communicate in space by the living body, which contains the possibilities of the living drawing in space: in the time and place. This research deals with the importance of the

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Publication Date
Thu Apr 01 2021
Journal Name
Computer Methods And Programs In Biomedicine
A hybrid approach based on multiple Eigenvalues selection (MES) for the automated grading of a brain tumor using MRI
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Publication Date
Tue Aug 23 2022
Journal Name
Frontiers In Energy Research
Evaluation of T-Shaped Fins With a Novel Layout for Improved Melting in a Triple-Tube Heat Storage System
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The effects of T-shaped fins on the improvement of phase change materials (PCM) melting are numerically investigated in vertical triple-tube storage containment. The PCM is held in the middle pipe of a triple-pipe heat exchanger while the heat transfer fluid flows through the internal and external pipes. The dimension effects of the T-shaped fins on the melting process of the PCM are investigated to determine the optimum case. Results indicate that while using T-shaped fins improves the melting performance of the PCM, the improvement potential is mainly governed by the fin’s body rather than the head. Hence, the proposed T-shaped fin did not noticeably improve melting at the bottom of the PCM domain; additionally, a flat fin is ad

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Publication Date
Wed Sep 01 2021
Journal Name
Nanomedicine Research Journal
Preparation, Characterization, Antimicrobial and Antitumor Activity of Chitosan Schiff base / PVA / PVP Au, Ag Nanocomposite in Treatment of Breast Cancer Cell Line
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Objective(s): Biocompatibility, non-toxicity, minimal allergenicity, and biodegradability are all characteristics of chitosan. Other biological properties of chitosan have been reported, including antitumor, antimicrobial and antioxidant activities. This research aim is the synthesis of drug compounds by preparation and characterization of polymer chitosan Schiff base and chitosan Schiff base / Poly vinyl alcohol / poly vinyl pyrrolidone Nanocomposite and study applications (anticancer cell line, antimicrobial agents). Methods: Chitosan Schiff base was prepared from the reaction of chitosan with carbonyl group of 4-nitro benzaldehyde. Polymer blend have been prepared by solution casting method. Chitosan Schiff base mixing with PVA and PVP

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Publication Date
Fri May 30 2025
Journal Name
Iraqi Journal Of Science
The study of Histone Deacetylases Immunoexpression in relation to Regulating Vascular Endothelial Growth Factor (VEGF) Implicated in Malignant Progression of Colorectal cancer
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Colorectal cancer is a malignant condition that can arise from multiple causative factors. It ranks second, behind lung cancer, as a leading cause of cancer-related deaths worldwide. Extensive research has been conducted to unravel the genetic underpinnings and molecular mechanisms underlying the development of colorectal cancer (CRC). However, epigenetic modifications of histones at the DNA level have become significantly involved in several malignant diseases such as CRC. Hence, this research sought to assess, for the first time locally, the immunoexpression of HDAC-1 and 3 in a group of colorectal patients. Additionally, we explored potential correlations between the expression of HDAC-1, 3 and VEGF. This retrospective study enco

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Changes in Serum Levels of Tumor Necrosis Factor-Alpha and Antioxidant status in Different Stages of Malignant Prostate Cancer Patients in Iraq
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Chronic inflammation can induce proliferative events and posttranslational DNA modifications in prostate tissue through oxidative stress. The present study was designed to evaluate the changes in serum levels of TNF-α, malomdialdehyde (MDA) and total antioxidant status (TAS) patients with different stages of malignant prostatic cancer (PCa) and benign prostatic hyperplasia (BPH). One hundred males (age range of 58-72 years) with different stages of malignant PCa were recruited from the Radiotherapy and Nuclear Medicine Teaching Hospital in Baghdad during the period from September 2010 to April 2011. The patients were categorized according to the 4 disease stages (I, II, III, and IV); 25 patients with benign prostatic hyperplasia (BPH)

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Publication Date
Sun Jan 01 2023
Journal Name
Aip Conference Proceedings
Surface enhanced Raman spectroscopy based sensitive and specific detection of vitamin D3, glycated hemoglobin, and serum lipid profile of breast cancer patients
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Considering the expanding frequency of breast cancer and high incidence of vitamin D3 [25(OH)D3] insufficiently, this investigate pointed to explain a relation between serum [25(OH)D3] (the sunshine vitamin) level and breast cancer hazard. The current study aimed to see how serum levels of each [25(OH)D3], HbA1c%, total cholesterol (TC), high density lipoprotein cholesterol (HDL-C), low density lipoprotein cholesterol (LDL-C), and triglyceride (TG) were affected a woman’s risk of getting breast cancer. In 40 healthy volunteers and 69 untreated breast cancer patients with clinical and histological evidence which include outpatients and hospitalized admissions patients at the Oncology Center, Medical City / Baghdad - Iraq. Venous blood samp

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