Preferred Language
Articles
/
bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
...Show More Authors

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.

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Sun Mar 06 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Benzimidazole Derivatives
...Show More Authors

In this paper the new starting material 2-(5-chloro-1H-benzo[d]imidazole-2-yl) aniline (1) was synthesized by the condensation reaction of 4-chloro-o-phenylenediamine and anthranilic acid .The new Mannich base derivatives were synthesized using formaldehyde and different secondary amines to synthesize a new set of benzimidazole derivatives(2-5). Also, the new Schiff-base derivatives (6-10) were synthesized from the reaction of compound (1) with various aromatic aldehydes and the closure-ring was done successfully using mercapto acetic acid to get the new thiazolidine derivatives(11-12).These new compounds were characterized using some physical techniques like:FT-IR Spectra and 1HNMR Spectra.

View Publication Preview PDF
Crossref
Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Polyimide Contain Heterocyclic
...Show More Authors

Novel heterocyclic polyimide 5(a,b) have been synthesized based on polyacrylic backbone. The synthetic route start with nucleophilic substitution of 2-amino, or 4-amino, pyridine 1(a,b) to the polyacryloyl chloride afforded poly substituted amide 2(a,b). Another nucleophilic substitution were carried with adipoyl chloride to form polyimide chloride 3(a,b). Treatment of 3(a,b) with hydrazine hydrate afforded acid hydrazide polyimide 4(a,b), which upon cyclocondensation with carbon disulfide gave the target heterocyclic polyimide. The synthesized compounds were identified by spectroscopic methods: FT-IR, 1H-NMR and 13C-NMR.

View Publication Preview PDF
Crossref
Publication Date
Sat Sep 30 2017
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis and Characterization of Tri-Composite Activated Carbon
...Show More Authors

Activated carbon loading with metals oxides is new adsorbents and catalyst, which seem very promising for desulfurization process. The present study deals with the preparation of three metals oxides loaded on activated carbon (AC). The tri composite of ZnO/NiO/CoO/AC was characterized by X-Ray Diffraction (XRD), X-Ray florescence (XRF), N2 adsorption for BET surface area, pore volume and Atomic Force Microscopy (AFM). The effect of calcination temperature is investigated. The best calcination temperature is 250oC based on the presence of phase, low weight loss and keep at high surface area. The surface area and pore volume of prepared tri composite are 932.97m2/g and 0.6031cm3/g respec

... Show More
View Publication Preview PDF
Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some New 1,3Oxazepine Derivatives
...Show More Authors

  In this study, Schiff's bases [S3,S4] were synthezied by condensation of N,N-dimethyl amino benzaldehyde with primary aromatic amine[N-(hydrazinyl methyl)benzamide]. These Sciff's bases were found to react with maleic anhydride and phthalic anhydride to give 1,3Oxazepine[S5,S6,S7,S8] in good yields.            The structures confired by m.p ,T.L.C.,FT.IR and 1H-NMR (of some of them).

View Publication Preview PDF
Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis and Characterization of Some New Pyrazole Derivatives
...Show More Authors

This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], thereaction of this compound with theiosemicarbazide ledto produce a new carbothioamide compound [V], Which was reacted with ethyl chloro acetate to yield thethioxoimidazolidin compound [VI]. The condensation reaction of this compound with different substituted aldehyde give new alkene derivatives[VII]a-d. The synthesized compounds were characterized by melting points , FT-IR ,1H-NMR and Mass spectroscopy .

Publication Date
Tue Oct 30 2018
Journal Name
Iraqi Journal Of Physics
Synthesis and characterization of nanocrystalline copper sulfide powders
...Show More Authors

Nanocrystalline copper sulphide (Cu2-xS) powders were synthesized by chemical precipitation from their aqueous solutions composed of different molar ratio of copper sulfate dehydrate (CuSO4.5H2O) and thiorea (NH2)2CS as source of Cu+2, S-2 ions respectively, and sodium ethylene diamine tetra acetic acid dehydrate (EDTA) as a complex agent. The compositions, morphological and structural properties of the nanopowders were characterized by energy dispersive spectroscopy (EDS), scanning electron microscope (SEM), and X-ray diffraction (XRD), respectively. The compositional results showed that the copper content was high and the Sulfur content was low for both CuS and Cu2S nanopowders. SEM images shows that all products consist of aggregate o

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Aug 17 2001
Journal Name
Molecular Crystals And Liquid Crysta
Synthesis, characterization and study of mesomorphic behavior of new bent and linear core compounds containing heterocyclic rings
...Show More Authors

The article presents the synthesis and liquid crystalline properties of some of new bent and linear core compounds containing a 1,3,4-oxadiazole, piperazine and thiazolidin-4-one rings as a central core. The new synthesized compounds were characterized by elemental analysis and FTIR, ¹HNMR and mass spectroscopy). The liquid crystalline properties were studied by polarized optical microscopy and differential scanning calorimetry. All Schiff bases compounds with 1,3,4-oxadiazole and piprzaine ring in central core presented liquid crystalline properties. The liquid crystallinity of compounds containing 1,3,4-oxadiazole and thiazolidin-4-one rings as a central core were found depending on the type of terminal substituents.

Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Synthesis, Characterization, Antibacterial study and Efficiency of Inhibition of New di-β-enaminone Ligand and its Complexes
...Show More Authors
Abstract<p>The new ligand [3,3’-(1,2-phenylenebis(azanediyl))bis(5,5-dimethylcyclohex-2-en-1-one)] (L) derived from 5,5-Dimethylcyclohexane-1,3-dione with 1,2-phenylenediamine was used to prepare a new chain of metal complexes of Mn(ii), Co(ii), Ni(ii), Cu(ii), Cd(ii) and Zn(ii) by inclusive formula [M(L)]Cl2. Characterized compounds on the basis of <sup>1</sup>H, <sup>13</sup>CNMR (for ligand (L)), FT-IR and U.V spectrum, melting point, molar conduct, %C, %H and %N, the percentage of the metal in complexes %M, Magnetic susceptibility, thermal studies (TGA), while its corrosion inhibition for (plain steel) in tap water is studied by weight loss. These measurements proved th</p> ... Show More
View Publication
Scopus (5)
Crossref (5)
Scopus Crossref
Publication Date
Sat Sep 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Design and Study of Fractal Optical Modulator for Infrared Transmitted Signal
...Show More Authors

The optical modulator was designed by using iterated function

systems (IFSs) by IFS Construction Kit program. The modulator was inserted into the optical system using ZEMAX optical design program. In this program, it is assumed that the modulator is made from one of Ø¢ the infrared transmitting materials. Eight materials at room temperature were used in this study; these are IRTRAN materials, Si, and Ge for the range of 3-9 l-lm.

Systems were evaluated and analyzed by using different criteria,

including spot diagram, modulation transfer function, and point spread function. The effect of optical modulator change with the chang of Ø¢ its material results in focusing of functions and frequencies as requ

... Show More
View Publication Preview PDF
Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some New Thiazine , Azetidine and Thiazolidine Compounds Containing 1,3,4Thiadiazole Moiety And Their Antibacterial Study
...Show More Authors

     2-amino-5-mercapto-1,3,4-thiadiazole [I] were prepared by the cyclization of thiosemecarbazide with carbon disulphide and anhydrous  sodium carbonate in ethanol as a solvent. The reaction of compound [I] with alkyl halides yielded 2- amino-5-thioalkyl-1,3,4- thiadiazole [II] and [III] . Compound [II] and [III] were reacted with different aromatic aldehydes to yieled 2-[(substituted benzyliden ) amino] -5- thioalkyl-1,3,4- thiadiazole [IV]a-c , [V]a-d and [VI]a-d .  Schiff ,s bases [IV]a-c , [V]a-d and [VI]a-d  were found to react with  2mercapto benzoic acid in the triethyl amine to give 3-[ 5-( alkylthio) -1,3,4- thiadiazol-2-yl] 2,3- dihydro- 2- (aryl) benzo [e] [1,3] thiazine -4-one [VII]a-

... Show More
View Publication Preview PDF