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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 Apr 26 2022
Journal Name
Journal Of Contemporary Medical Sciences
Doxorubicin Immobilization on chitosan-modified silver Nanoparticles as a drug delivery method for effective anticancer treatment
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Objective: The goal of this research is to load Doxorubicin (DOX) on silver nanoparticles coupled with folic acid and test their anticancer properties against breast cancer. Methods: Chitosan-Capped silver nanoparticles (CS-AgNPs) were manufactured and loaded with folic acid as well as an anticancer drug, Doxorubicin, to form CS-AgNPs-DOX-FA conjugate. AFM, FTIR, and SEM techniques were used to characterize the samples. The produced multifunctional nano-formulation served as an intrinsic drug delivery system, allowing for effective loading and targeting of chemotherapeutics on the Breast cancer (AMJ 13) cell line. Flowcytometry was used to assess therapy efficacy by measuring apoptotic induction.  Results: DOX and CS-Ag

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Publication Date
Fri Apr 01 2022
Journal Name
Chemical Methodologies
Design, Synthesis of Imidazolone and Oxazepine Derivatives Bearing Imidazo (2, 1-b) Thiazole along with its Antimicrobial Activity
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A new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal a

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Publication Date
Wed Jan 01 2020
Journal Name
International Conference Of Numerical Analysis And Applied Mathematics Icnaam 2019
Isolation and characterization study towards microbial improved oil recovery applications
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Publication Date
Thu Aug 17 2023
Journal Name
Journal Of Thermoplastic Composite Materials
Fabrication and characterization of PEKK nanocomposites: An in vitro study
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Although the number of implants has increased gradually and consistently over the years to around one million per year globally, there is still far more potential for advancement in the field of dental implantology which is typically growing quickly. This study investigates the effect of nanofiller reinforcement high-performance polymer matrix to enhance mechanical and physical characteristics. Calcium silicate (CS)/Polyetherketoneketone (PEKK) biomedical composite (G0 as a control group) is reinforced with different weight percentages (G1-G4) of tellurium dioxide nanoparticles (TeO2NPs) ( n = 5). This research uses ethanol as a binder for mixing various weight percentages (wt%) of TeO2NPs w

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis and characterization of mixed ligand complexes of 8- hydroxy quinoline and Schiff base with some metal ions
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A new mixed ligand complexes have been prepared between 8- hydroxy quinoline and o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on with Mn(II),Fe(II),Co(II),Ni(II) and Cu(II) ions . the prepared complexes were isolated and characterized by (FT-IR)and (UV-Vis) spectroscopy. Elemental analysis (C.H.N) Flame atomic absorption technique . in addition to magnetic susceptibility and conductivity measurement.

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and characterization of some heterocyclic including oxazoles,Thiazoles, Pyridazines, phthalizines and Pyrazoles with evaluating of biological activity.
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A series of new compounds including p-bromo methyl pheno acetate [2]. N-( aminocarbonyl)–p-bromo pheno acetamide [3] , N-( aminothioyl) -p-bromo phenoacetyl amide [4], N-[4-(p-di phenyl)-1,3-oxazol-2-yl]-p-bromopheno acetamide [5],N-[4-p-di phenyl]-1,3-thiazol-2-yl-p-bromo phenoacet amide [6], p-bromopheno acetic acid hydrazide [7] , 1-N-(p-bromo pheno acetyl)-1,2-dihydro-pyridazin-3,6- dione [8], 1-N-(p-bromo pheno acetyl)-1,2-dihydro-phthalazin-3,8- dione[ 9], 1-(p-bromo pheno acetyl)-3-methylpyrazol-5-one [10] and 1-(p-bromo phenol acetyl)- 3,5-dimethyl pyrazole [11] have been synthesized. The prepared compounds were characterized by m.p.,FT-IR and 1H-NMR spectroscopy. Also ,the biological activity was evaluated .

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Publication Date
Fri Dec 29 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of 1, 3-Oxazepine and Benz [1, 2-e][1, 3] Oxazepine-4, 7-Diones
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N-Benzylidene m-nitrobenzeneamines (Schiff bases) were prepared by condensation of m-nitroaniline with aromatic aldehydes. These Schiff bases were found to react with maleic anhydride to give 2-Aryl-3-(m-nitrophenyl)-2, 3-dihydro [1, 3] oxazepine–4, 7–diones and with phthalic anhydride to give 2-Aryl-3–(m-nitrophenyl)–2, 3–dihydrobenz|| 1, 2-e|||| 1, 3] oxazepine–4, 7-diones which were reacted with pyrrolidine to give the anilide–pyrrolidides of maleic acid and phthalic acid.

Publication Date
Sun Jan 01 2012
Journal Name
Third Scientific Conference / College Of Science - University Of Diyala -2012 A Scientific Referred Journal Published By College Of Science University Of Diyala July
Synthesis, Characterization, Schiff Base phenyl2-(2-hydroxybenzylidenamino)benzoate and its complexes with Pr III , Cr and IIILa , III
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The aim of the work is the synthesis and characterization of the tridentate Schiff base (HL) containing (N and O) as donor atoms type (ONO). The ligand is: (HL) phenyl 2-(2-hydroxybenzylidenamino)benzoate This ligand was prepared by the reaction of (phenyl 2-aminobenzoate) with salicylaldehyde under reflux in ethanol and few drops of glacial acetic acid which gave the ligand (HL). The prepared ligand was characterized by (FT IR,UV–Vis) spectroscopy, Elemental analysis of carbon, hydrogen and nitrogen (C.H.N.) and melting point. The ligand was reacted with some metal ions under reflux in ethanol with (1 metal :2 ligand )mole ratio which gave complexes of the general formula: Pr III , Cr and III La III [M(L)2]Cl , M = Products were found to

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Publication Date
Wed Sep 05 2018
Journal Name
Journal Of Education And Scientific Studies
Ligand-Mixed New of Evaluation Bacterial and Characterization ,Synthesis Some with phenanthroline1,10- and Dithiocarbamate Containing Complexes ions M
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(phen) (L(M [formula general a with complexes ligand-mixed new of series A methods analyses different by characterised and synthesised been have ,ligand arysecond as phenanthroline1,10- = phen and ligand primary as dithiocarbamate-1-azolebenzoimid-H-1)sulfinyl)methyl)yl-”-2pyriden)trifluroethoxy2,2,2- “(-4-methyl3-(((2-Sodium = L,ZnIIandCdII,CuII,NiII,CoII= M where,Cl)]phen)(L(Pd [Cland]2)O2H( ligands to metal ,moments magnetic and ,elementalanalysis ,spectrum mass ,surementsmea conductivity ,analysis thermal ,spectroscopy Vis-UV ,IR-FT ,NMR-C,13 H1 such dithiocarbamate the with formed coordination anisobidentate that showed spectra IRFT The.)phen:dithiocarbamate:M) (1:1:1(be to found been has complexes all in ratio nitrogen th

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Publication Date
Tue Jan 01 2013
Journal Name
Al- Mustansiriyah J. Sci.
Synthesis and Characterization of Some Mixed Ligand Complexes of Quinaldic Acid and α-Picoline with Some Metal Salts
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Some metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato

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