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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
Tue Oct 21 2014
Journal Name
Diyala Journal For Pure Sciences
synthesis and characterization of New schiff base Ligand Derived from 4-amino anti pyrine and it's complexes with some Metal lons and theirAntibacterial studies
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synthesis and characterization of New schiff base Ligand Derived from 4-amino anti pyrine and it's complexes with some Metal lons and theirAntibacterial studies

Publication Date
Sat Sep 01 2018
Journal Name
International Journal Of Applied Pharmaceutics
PREPARATION AND CHARACTERIZATION OF ECONAZOLE NITRATE INCLUSION COMPLEX FOR OCULAR DELIVERY SYSTEM
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Objective: Econazole nitrate (ECZ) is one of the triazole antifungal drugs with poor aqueous solubility and dissolution rate; there is a need for enhancement of solubility. Therefore; inclusion complexation with β cyclodextrin (βCD) was performed. Methods: In this study kneading method and co-evaporation method of preparation of inclusion complex between βCD and ECZ using two molar ratios of βCD. The solubility of these complexes in isotonic saline solution and distilled water was studied. Complexes prepared by kneading method were used for the preparation of different ophthalmic gel formulas using carbomer (CB) and sodium carboxymethylcellulose (sod CMC) as a gelling agent. The release profile and the rheological behaviour of the gel w

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Publication Date
Wed Jan 01 2025
Journal Name
Opennano
Development and characterization of bilastine nanosuspension for enhanced dissolution in orodispersible films
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Abstract Bilastine, a second-generation antihistamine, is commonly prescribed for managing allergic rhinoconjunctivitis and urticaria due to its prolonged action. However, its therapeutic potential is constrained by poor water solubility and low oral bioavailability. This study aimed to enhance bilastine dissolution and patient compliance by formulating a nanosuspension-based orodispersible film (ODF). An anti-solvent precipitation method was employed to produce nanosuspension using different hydrophilic stabilizers (Soluplus®, Poloxamer 188, and PEG 6000). The influence of formulation parameters, such as the stabilizer ratio, the anti-solvent ratio, stirring speed, and the stabilizer type, on particle size and polydispersity index (PDI)

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Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
The Preparing and Characterization of Nanocomposite (PTh/SWCNT) for NO2 Gas Sensing
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We prepared polythiophene (PTH) with single wall carbon nanotube (SWCNT) nanocomposite thin films for Nitrogen dioxide (NO2) gas sensing applications. Thin films were synthesized via electrochemical polymerization method onto (Indium tin oxide) ITO coated glass substrate of thiophene monomer with magnesium perchlorate and different concentration from SWCNT (0.012 and 0.016) % in the presence130mL of Acetonitrile used. X-ray diffraction (XRD), Field Emission Scanning Electron microscopy (FE-SEM), Atomic Force Microscope (AFM) and Fourier Transform Infrared Spectroscopy (FT-IR) were used to characterized these nanocomposite thin films. The response of these nanocomposite for NO2 gas was evaluated via monitoring the change

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Publication Date
Wed Dec 01 2021
Journal Name
Baghdad Science Journal
Fabrication and Characterization of Nanofibers Membranes using Electrospinning Technology for Oil Removal
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Oily wastewater is one of the most challenging streams to deal with especially if the oil exists in emulsified form. In this study, electrospinning method was used to prepare nanofiberous polyvinylidene fluoride (PVDF) membranes and study their performance in oil removal. Graphene particles were embedded in the electrospun PVDF membrane to enhance the efficiency of the membranes. The prepared membranes were characterized using a scanning electron microscopy (SEM) to verify the graphene stabilization on the surface of the membrane homogeneously; while FTIR was used to detect the functional groups on the membrane surface. The membrane wettability was assessed by measuring the contact angle. The PVDF and PVDF / Graphene membranes efficiency

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation, Characterization and Prophylactic Study of New Microsphere Containing Doxycycline against Diseases of Shrimp
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Therapeutically and prophylactically using Microspheres containing doxycycline isolated from shell of shrimp. Low molecule weight poly lactic acid was prepared. In this study, Poly lactic acid (PLA)/ poly vinyl alcohol (PVA)/poly ethyleneglycol(PEG) loading doxycycline blend solutions was prepared. Also Poly lactic acid (PLA)-Tannin blend via solvent evaporation method was prepared. Microspheres of chitosan/gelatin microsphere loading doxycycline was prepared by emulsion crosslinking technique. Both microsphere and blends were characterized by Fourier transform infrared (FTIR) spectrophotometer. The FTIR spectra were shown distinguish bands. The in vitro release of doxcycline from its matrix at pH 7 was studied. The prophylactic

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Publication Date
Thu Apr 27 2023
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn: 2789-3219 )
Anticancer Activities of Some Heterocyclic Compounds Containing an Oxygen Atom: A Review
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The purpose of this study is to underline the progression and development of research regarding oxygen-containing heterocycles as well as the contribution that some oxygen-containing heterocycles have made as anticancer medicines. A series of publications about the antitumor effects of derivatives of heterocyclic compounds containing an oxygen atom, such as furan, benzofuran, oxazole, benzoxazole, and oxadiazole, were evaluated, and their anticancer activities showed encouraging results when compared to those of established standard treatments.

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Publication Date
Sat Mar 20 2021
Journal Name
Neuroquantology
XRD and Microscopic Images for Synthesis Graphite Nanoparticles by Oxidation Method
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Graphite nanoparticles were successfully synthesized using mixture of H2O2/NH4OH with three steps of oxidation. The process of oxidations were analysis by XRD and optics microscopic images which shows clear change in particle size of graphite after every steps of oxidation. The method depend on treatments the graphite with H2O2 in two steps than complete the last steps by reacting with H2O2/NH4OH with equal quantities. The process did not reduces the several sheets for graphite but dispersion the aggregates of multi-sheets carbon when removed the Van Der Waals forces through the oxidation process.

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Publication Date
Thu Sep 13 2018
Journal Name
Baghdad Science Journal
Synthesis and Fabrication of In2O3: CdO Nanoparticles for NO2 Gas Sensor
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The physical and morphological characteristics of porous silicon (PS) synthesized via gas sensor was assessed by electrochemical etching for a Si wafer in diluted HF acid in water (1:4) at different etching times and different currents. The morphology for PS wafers by AFM show that the average pore diameter varies from 48.63 to 72.54 nm with increasing etching time from 5 to 15min and from 72.54 to 51.37nm with increasing current from 10 to 30 mA. From the study, it was found that the gas sensitivity of In2O3: CdO semiconductor, against NO2 gas, directly correlated to the nanoparticles size, and its sensitivity increases with increasing operating temperature.

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Publication Date
Wed Aug 28 2019
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Screening their Antibactrial Activity of some New Oxazepine and Diazepine Compounds Containing 1,3,4-Oxadiazole Ring Derived from L-Ascorbic Acid
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The search involve the synthesis of some new 1,3-oxazepine and 1,3-diazepine derivatives were synthesized from Schiff base. The Schiff base (VIII) prepared from reaction of aldehyde (IV) derived from L-ascorbic acid with aromatic amine ([2-(4- nitrophenyl)-5-(4-aminophenyl)-1,3,4-oxadiazole] (VII). Oxazepine compounds (IX-XI) were synthesized from the cyclic condensation of Schiff base (VIII) with (maleic, phthalic and 3-nitrophthalic) anhydride, compounds (IX-XI) that were reacted with p-methoxyaniline to give diazepine derivatives (XII-XIV). The structures of the new synthesized compounds have been confirmed by physical properties and spectroscopy measurements such as FTIR, and some of them by 1 H-NMR, 13 CNMR, Mass, and evaluated

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