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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 Mar 09 2017
Journal Name
Sensors
A Multimodality Hybrid Gamma-Optical Camera for Intraoperative Imaging
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The development of low profile gamma-ray detectors has encouraged the production of small field of view (SFOV) hand-held imaging devices for use at the patient bedside and in operating theatres. Early development of these SFOV cameras was focussed on a single modality—gamma ray imaging. Recently, a hybrid system—gamma plus optical imaging—has been developed. This combination of optical and gamma cameras enables high spatial resolution multi-modal imaging, giving a superimposed scintigraphic and optical image. Hybrid imaging offers new possibilities for assisting clinicians and surgeons in localising the site of uptake in procedures such as sentinel node detection. The hybrid camera concept can be extended to a multimodal detec

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Publication Date
Fri Mar 31 2023
Journal Name
Journal Of Al-qadisiyah For Computer Science And Mathematics
A Cryptosystem for Database Security Based on RC4 Algorithm
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Because of vulnerable threats and attacks against database during transmission from sender to receiver, which is one of the most global security concerns of network users, a lightweight cryptosystem using Rivest Cipher 4 (RC4) algorithm is proposed. This cryptosystem maintains data privacy by performing encryption of data in cipher form and transfers it over the network and again performing decryption to original data. Hens, ciphers represent encapsulating system for database tables

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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)
Guggulusome - A Novel Vesicular Carriers for Enhanced Transdermal Delivery
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The present work describes guggul as a novel carrier for some anti-inflammatory drugs. Guggulusomes containing different concentration of guggul with aceclofenac were prepared by sonication method and characterized for vesicle shape, size, size-distribution, pH, viscosity, spread ability, homogeneity, and accelerated stability in-vitro drug permeation through mouse skin. The vesicles exhibited an entrapment efficiency of 93.2 ± 12%, vesicle size of 0.769 ± 3μm and a zeta potential of - 6.21mV. In vitro drug release was analyzed using Franz’s diffusion cells. The cumulative release of the guggulusomes gel (G2) was 75.8% in 18 hrs, which is greater than that all the gel formulation. The stability profile of prepare

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Publication Date
Thu May 17 2012
Journal Name
Eurasip Journal On Wireless Communications And Networking
A cluster-based proxy mobile IPv6 for IP-WSNs
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Publication Date
Sat Aug 06 2022
Journal Name
Ijci. International Journal Of Computers And Information
Techniques for DDoS Attack in SDN: A Comparative Study
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Abstract Software-Defined Networking (commonly referred to as SDN) is a newer paradigm that develops the concept of a software-driven network by separating data and control planes. It can handle the traditional network problems. However, this excellent architecture is subjected to various security threats. One of these issues is the distributed denial of service (DDoS) attack, which is difficult to contain in this kind of software-based network. Several security solutions have been proposed recently to secure SDN against DDoS attacks. This paper aims to analyze and discuss machine learning-based systems for SDN security networks from DDoS attack. The results have indicated that the algorithms for machine learning can be used to detect DDoS

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Publication Date
Mon May 11 2020
Journal Name
Baghdad Science Journal
A Cryptosystem for Database Security Based on TSFS Algorithm
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Implementation of TSFS (Transposition, Substitution, Folding, and Shifting) algorithm as an encryption algorithm in database security had limitations in character set and the number of keys used. The proposed cryptosystem is based on making some enhancements on the phases of TSFS encryption algorithm by computing the determinant of the keys matrices which affects the implementation of the algorithm phases. These changes showed high security to the database against different types of security attacks by achieving both goals of confusion and diffusion.

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Publication Date
Sat Oct 01 2016
Journal Name
International Journal Of Pure And Apllied Mathematics
A SEMI ANALYTICAL ITERATIVE TECHNIQUE FOR SOLVING DUFFING EQUATIONS
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Publication Date
Fri Dec 01 2017
Journal Name
Journal Of Computational And Theoretical Nanoscience
Three-Dimensional Seismic Response Analysis for a Rockfill Dam
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Publication Date
Sat Jul 01 2017
Journal Name
Journal Of King Saud University - Science
A semi-analytical iterative technique for solving chemistry problems
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Publication Date
Tue Jun 08 2021
Journal Name
Biomolecules
A Pan-Inhibitor for Protein Arginine Methyltransferase Family Enzymes
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Protein arginine methyltransferases (PRMTs) play important roles in transcription, splicing, DNA damage repair, RNA biology, and cellular metabolism. Thus, PRMTs have been attractive targets for various diseases. In this study, we reported the design and synthesis of a potent pan-inhibitor for PRMTs that tethers a thioadenosine and various substituted guanidino groups through a propyl linker. Compound II757 exhibits a half-maximal inhibition concentration (IC50) value of 5 to 555 nM for eight tested PRMTs, with the highest inhibition for PRMT4 (IC50 = 5 nM). The kinetic study demonstrated that II757 competitively binds at the SAM binding site of PRMT1. Notably, II757 is selective for PRMTs over a panel of other methyltransferases, w

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