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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
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Isradipine as Oral Nanoemulsion
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        Isradipine related to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used to treat hypertension, angina pectoris, as well as Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, thus, oral bio-availability will be approximately15 to 24 %. 

       The aim of the study is preparing stable oral oil in water (o/w) nanoemulsion of isradipine to promote the colloidial dispersion of isradipine in the nano range, so that it may be absorded by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism (israpidi

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Publication Date
Mon Jul 01 2024
Journal Name
Russian Journal Of Organic Chemistry
Synthesis and Study of the Biological Activity of New Compounds Derived from 4-(5-Phenyl-1,3,4-oxadiazole-2-yl)aniline
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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Theoretical Study of 4-(2-methyl-4-oxoquinazoline-3(4H)-yl) Benzoic acid with Some Transition Metal Ions
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New complexes of the type [ML2(H2O)2] ,[FeL2(H2O)Cl] and [VOL2] were M=Co(II),Ni(II) and Cu(II) ,L=4-(2-methyl-4-oxoquinazoline-3(4H)-yl) benzoic acid were synthesized and characterized by element analysis, magnetic susceptibility ,molar conductance ,FT-IR and UV-visible. The studies indicate that the L acts as doubly monodentate bridge for metal ions and form mononuclear complexes. The complexes are found to be octahedral except V(IV) complex is square pyrimde shape . The structural geometries of compounds were also suggested in gas phase by theoretical treatments, using Hyper chem-6 program for the molecular mechanics and semi-empirical calculations, addition heat of formation(?Hf ?) and binding energy (?Eb)for the free ligan

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Publication Date
Fri Sep 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Antibacterial, and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives using Vilsmeier Reagent
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Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacteri

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Publication Date
Thu Jul 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Antibacterial and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives Using Vilsmeier Reagen
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Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activit

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Publication Date
Sat Jan 01 2022
Journal Name
Results In Chemistry
Interfacial polymerization synthesis of polypyrrole and sodium metavanadate (PPy/NaVO3) composite as an excellent performance electrode for supercapacitors
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Herein, the interfacial polymerization method has been used for the synthesis of PPy/NaVO3 composites with different compositions of NaVO3 (10 %, 20 %, 30 %, 40 % and 50 %) as an efficient electrode material for supercapacitors. The successful formation and composition of the as-prepared composites (PV1-PV5) were confirmed by FTIR, XRD, EDX, and SEM analysis. The electrochemical properties were investigated by cyclic voltammetry (CV), galvanometric charge–discharge measurement (GCD), and electrochemical impedance spectroscopy (EIS) in 0.5 M H2SO4 electrolyte. As compared to other, the PV4 composite exhibit excellent specific capacitance of 391 F g−1 at a current density of 0.75 A/g with good cycling stability of ∼59 % after 1000 cycle

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Publication Date
Fri Sep 01 2017
Journal Name
Journal Of Construction Engineering And Management
Integrating Worker Health and Safety into Sustainable Design and Construction: Designer and Constructor Perspectives
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Publication Date
Thu Sep 01 2022
Journal Name
Journal Of Stomatology
The effectiveness of limited flap design in surgical removal of fully impacted lower third molars: a comparative clinical study
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Publication Date
Wed Oct 20 2010
Journal Name
The International Journal Of Advanced Manufacturing Technology
Finite element modeling and simulation of proposed design magneto-rheological valve
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Magneto-rheological (MR) valve is one of the devices generally used to control the speed of Hydraulic actuator of MR fluid. The performance of valve depends on the magnetic circuit design. Present study deals with a new design of MR valve. A mathematical model for the MR valve is developed and the simulation is carried out to evaluate the newly developed MR valve. The design of the magnetic circuit is accomplished by magnetic finite element software such as Finite Element Method Magnetic (FEMMR). The model dimensions of MR valve, material properties are taken into account. The results of analysis are presented in terms of magnetic strength H and magnetic flux density B. The simulation results based on the proposed model indicate that the ef

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Publication Date
Wed Sep 10 2014
Journal Name
International Journal Of Computer Applications
Design and Implementation of Appliance Controller using Traditional or Smart Phone
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Mobile phones are widely used nowadays, for different application such as wireless control and monitoring due to its availability and ease of use. The implemented system is based on "global system mobile (GSM)" network by using "short message service (SMS)". The design mainly contains a GSM modem and interfacing unit circuit with microcontrollers. This system could control up to eight different electrical devices such as light, Air conditioner, washing machine and many more applications which needed in daily life in different area (House, Office, or factory, etc.). The control is done by sending a specific SMS messages from traditional or smart phone. The controlling devices are restricted to a pre-defined phone number and are set in the so

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