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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 Dec 01 2022
Journal Name
Journal Of Engineering
Deep Learning-Based Segmentation and Classification Techniques for Brain Tumor MRI: A Review
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Early detection of brain tumors is critical for enhancing treatment options and extending patient survival. Magnetic resonance imaging (MRI) scanning gives more detailed information, such as greater contrast and clarity than any other scanning method. Manually dividing brain tumors from many MRI images collected in clinical practice for cancer diagnosis is a tough and time-consuming task. Tumors and MRI scans of the brain can be discovered using algorithms and machine learning technologies, making the process easier for doctors because MRI images can appear healthy when the person may have a tumor or be malignant. Recently, deep learning techniques based on deep convolutional neural networks have been used to analyze med

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Publication Date
Wed Mar 01 2023
Journal Name
Journal Of Engineering
Recycled Concrete Aggregated for the use in Roller Compacted Concrete: A Literature Review
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The using of recycled aggregates from construction and demolition waste (CDW) can preserve natural aggregate resources, reduce the demand for landfill, and contribute to a sustainable built environment. Concrete demolition waste has been proven to be an excellent source of aggregates for new concrete production. At a technical, economic, and environmental level, roller compacted concrete (RCC) applications benefit various civil construction projects. Roller Compacted Concrete (RCC) is a homogenous mixture that is best described as a zero-slump concrete placed with compacting equipment, uses in storage areas, dams, and most often as a basis for rigid pavements. The mix must be sufficiently dry to support

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Publication Date
Tue Oct 01 2019
Journal Name
Biochemical & Cellular Archives
A RE-SATURATION IMPACT ON SOIL RETENTION CURVE FOR FIVE DIFFERENT TEXTURED SOILS
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Soil water retention curves (SWRCs) are crucial for characterizing soil moisture dynamics and are particularly relevant in the context of irrigation management. A study was carried out to obtain the SWRC, inflection point, S index, pore size distribution curve, macro porosity, and air capacity from samples submitted to saturation and re-saturation processes. Five different-texture disturbed soil samples Sandy Loam, Loam, Sandy Clay Loam, Silt Loam, and Clay were collected. After obtaining SWRC, each air-dried soil samples were submitted to particle size distribution and clay dispersed in water analyses to verify the soil lost clay. The experimental design was completely randomized with three replications using two processes of SWRC (saturat

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Publication Date
Thu Jun 01 2023
Journal Name
Bulletin Of Electrical Engineering And Informatics
A missing data imputation method based on salp swarm algorithm for diabetes disease
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Most of the medical datasets suffer from missing data, due to the expense of some tests or human faults while recording these tests. This issue affects the performance of the machine learning models because the values of some features will be missing. Therefore, there is a need for a specific type of methods for imputing these missing data. In this research, the salp swarm algorithm (SSA) is used for generating and imputing the missing values in the pain in my ass (also known Pima) Indian diabetes disease (PIDD) dataset, the proposed algorithm is called (ISSA). The obtained results showed that the classification performance of three different classifiers which are support vector machine (SVM), K-nearest neighbour (KNN), and Naïve B

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Publication Date
Wed Sep 29 2021
Journal Name
Molecules
A Comprehensive Review for Groundwater Contamination and Remediation: Occurrence, Migration and Adsorption Modelling
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The provision of safe water for people is a human right; historically, a major number of people depend on groundwater as a source of water for their needs, such as agricultural, industrial or human activities. Water resources have recently been affected by organic and/or inorganic contaminants as a result of population growth and increased anthropogenic activity, soil leaching and pollution. Water resource remediation has become a serious environmental concern, since it has a direct impact on many aspects of people’s lives. For decades, the pump-and-treat method has been considered the predominant treatment process for the remediation of contaminated groundwater with organic and inorganic contaminants. On the other side, this tech

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Publication Date
Tue Aug 06 2013
Journal Name
Robotica
Function approximation technique-based adaptive virtual decomposition control for a serial-chain manipulator
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SUMMARY<p>The virtual decomposition control (VDC) is an efficient tool suitable to deal with the full-dynamics-based control problem of complex robots. However, the regressor-based adaptive control used by VDC to control every subsystem and to estimate the unknown parameters demands specific knowledge about the system physics. Therefore, in this paper, we focus on reorganizing the equation of the VDC for a serial chain manipulator using the adaptive function approximation technique (FAT) without needing specific system physics. The dynamic matrices of the dynamic equation of every subsystem (e.g. link and joint) are approximated by orthogonal functions due to the minimum approximation errors produced. The contr</p> ... Show More
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Publication Date
Fri Jul 21 2023
Journal Name
Journal Of Engineering
A Modified 2D-Checksum Error Detecting Method for Data Transmission in Noisy Media
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In data transmission a change in single bit in the received data may lead to miss understanding or a disaster. Each bit in the sent information has high priority especially with information such as the address of the receiver. The importance of error detection with each single change is a key issue in data transmission field.
The ordinary single parity detection method can detect odd number of errors efficiently, but fails with even number of errors. Other detection methods such as two-dimensional and checksum showed better results and failed to cope with the increasing number of errors.
Two novel methods were suggested to detect the binary bit change errors when transmitting data in a noisy media.Those methods were: 2D-Checksum me

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Publication Date
Thu Dec 01 2016
Journal Name
Swarm And Evolutionary Computation
A new multi-objective evolutionary framework for community mining in dynamic social networks
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Publication Date
Mon Jul 01 2019
Journal Name
International Journal Of Heat And Mass Transfer
Hybrid heat transfer enhancement for latent-heat thermal energy storage systems: A review
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Publication Date
Sun Apr 30 2017
Journal Name
Journal Of Engineering
Experimental Study on Heat Transfer and Friction Factor Characteristics of Single Layer Graphene Based DI-water Nanofluid in a Circular Tube under Laminar Flow and Different Heat Fluxes as Boundary Conditions
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An experimental study was performed to estimate the forced convection heat transfer performance and the pressure drop of a single layer graphene (GNPs) based DI-water nanofluid in a circular tube under a laminar flow and a uniform heat flux boundary conditions. The viscosity and thermal conductivity of nanofluid at weight concentrations of (0.1 to 1 wt%) were measured. The effects of the velocity of flow, heat flux and nanoparticle weight concentrations on the  enhancement of the heat transfer are examined. The Nusselt number of the GNPs nanofluid was enhanced as the heat flux and the velocity of flow rate  increased, and the maximum Nusselt number  ratio (Nu nanofluid/ Nu base fluid)   and thermal performance factor

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