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bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple  drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed  towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of  two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis  of the target compounds was  accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed  that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug  selectively  into the cancer cells to be hydrolyzed by enzymes that are elevated in  tumor tissues compared with normal tissues .

Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.

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Publication Date
Sun Jun 30 2013
Journal Name
International Journal For Sciences And Technology
Synthesis and anti-bacterial study of novel compounds with bis (four-, five-, and seven-membered) heterocyclic rings
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New twin compounds having four-, five-, and seven- membered heterocyclic rings were synthesized via Schiff bases (1a,b) which were obtained by the condensation of o-tolidine with two moles of 4- N,N-dimethyl benzaldehyde or 4- chloro benzaldehyde. The reaction of these Schiff bases with two moles of phenyl isothiocyanate, phenyl isocyanate or naphthyl isocyanate as in scheme(1) led to the formation of bis -1,3- diazetidin- 2- thion and bis -1,3- diazetidin -2-one derivatives (2-4 a,b). While in scheme (2) bis imidazolidin-4-one (5a,b) ,bistetrazole (6a,b) and bis thiazolidin-4-one (7a,b) derivatives were produced by reacting the mentioned Schiff bases(1a,b)with two moles of glycine, sodium azide or thioglycolic acid, respectively. The new b

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Publication Date
Tue Dec 22 2020
Journal Name
Lecture Notes In Civil Engineering
Proposed Design Charts for Reinforced Concrete Spread Foundations Subjected to Concentric Load
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The design of reinforced concrete spread foundations mainly depends on soil bearing capacity, loading value, and column size. So for each design case, tiresome calculations and time consumption are needed. In this paper, generalized design charts are presented and plotted according to derivations based on the ACI 318 M-2019 Code. These charts could be used directly by the structural designers to estimate the column size, foundation thickness, and dimensions as well as the foundation reinforcement under a certain given concentric load assuming a uniformly distributed contact pressure underneath the foundation. Of noteworthy, these charts are oriented to deal with square isolated footings with a square concentric column, covering reasonable r

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Publication Date
Mon Apr 02 2018
Journal Name
Al-nahrain Journal For Engineering Sciences (njes)
Output Feedback Adaptive Sliding Mode Control Design for a Plate Heat Exchanger
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The heat exchanger is a device used to transfer heat energy between two fluids, hot and cold. In this work, an output feedback adaptive sliding mode controller is designed to control the temperature of the outlet cold water for plate heat exchanger. The measurement of the outlet cold temperature is the only information required. Hence, a sliding mode differentiator was designed to estimate the time derivative of outlet hot water temperature, which it is needed for constructing a sliding variable. The discontinuous gain value of the sliding mode controller is adapted according to a certain adaptation law. Two constraints which imposed on the volumetric flow rate of outlet cold (control input) were considered within the rules of the proposed

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Publication Date
Wed Jun 06 2001
Journal Name
المجلة العراقية للعلوم الاحصائية
Suggest formulas for estimating carry-over effects in two-period changeover design
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This research aims to suggest formulas to estimate carry-over effects with two-period change-over design, and then, all other effects in the analysis of variance of this design, and find the efficiency of the two-period change-over design relative to another design (say, completely randomized design).

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Publication Date
Fri Jan 01 2016
Journal Name
5th Iet International Conference On Renewable Power Generation (rpg), 2016, London, Uk
Electrical Machine Design for use in an External Combustion Free Piston Engine
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Publication Date
Sun Aug 01 2021
Journal Name
Journal Of Mechanical Engineering Research And Developments
Slot Design Procedure for a NACA 4412 at High Angle of Attack
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The main objective of the present work is to find a method increases the efficiency of the airfoil that is used for blade in wind turbine, wing in aircraft, propeller and helicopter (like NACA 4412). By overcoming the separation of flow at high angle of attacks, a slotted airfoil had been used and solved numerically through connecting the pressure side in the bottom surface with the suction side in the top surface of the airfoil to energize the separated flow. Slot exit, width and slope were considered as a parameters of slot configuration to determine the effective design of consideration. Reynolds number was taken as [1.6 x106 ] and the angle of attacks were ranged from (0o - 20o ). The numerical solution with Ansys Fluent commercial prog

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Publication Date
Wed Jul 01 2020
Journal Name
Journal Of Engineering
Bat Algorithm Based an Adaptive PID Controller Design for Buck Converter Model
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The aim of this paper is to design a PID controller based on an on-line tuning bat optimization algorithm for the step-down DC/DC buck converter system which is used in the battery operation of the mobile applications. In this paper, the bat optimization algorithm has been utilized to obtain the optimal parameters of the PID controller as a simple and fast on-line tuning technique to get the best control action for the system. The simulation results using (Matlab Package) show the robustness and the effectiveness of the proposed control system in terms of obtaining a suitable voltage control action as a smooth and unsaturated state of the buck converter input voltage of ( ) volt that will stabilize the buck converter sys

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Publication Date
Sat Dec 01 2018
Journal Name
2018 Third Scientific Conference Of Electrical Engineering (scee)
An Intelligent Cognitive System Design for Mobile Robot based on Optimization Algorithm
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Publication Date
Thu Dec 28 2023
Journal Name
Journal Européen Des Systèmes Automatisés
Design of a Hybrid Adaptive Controller for Series Elastic Actuators of Robots
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Publication Date
Thu Oct 01 2020
Journal Name
International Journal Of Electrical And Computer Engineering (ijece)
Design of an adaptive state feedback controller for a magnetic levitation system
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This paper presents designing an adaptive state feedback controller (ASFC) for a magnetic levitation system (MLS), which is an unstable system and has high nonlinearity and represents a challenging control problem. First, a nonadaptive state feedback controller (SFC) is designed by linearization about a selected equilibrium point and designing a SFC by pole-placement method to achieve maximum overshoot of 1.5% and settling time of 1s (5% criterion). When the operating point changes, the designed controller can no longer achieve the design specifications, since it is designed based on a linearization about a different operating point. This gives rise to utilizing the adaptive control scheme to parameterize the state feedback controll

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