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.
Two Schiff base ligands L1 and L2 have been obtained by condensation of salicylaldehyde respectively with leucylalanine and glycylglycine then their complexes with Zn(II)were prepared and characterized by elemental analyses , conductivity measurement , IR and UV-Vis .The molar conductance measurement indicated that the Zn(II) complexes are 1:1 non-electrolytes. The IR data demonstrated that the tetradentate binding of the ligands L1 and L2 . The in vitro biological screening effect of the investigated compounds have been tested against the bacterial species Staphlococcus aureus, Escherichia coil , Klebsiella pneumaniae, Proteus vulgaris and Pseudomonas aeruginosa by the disc diffusion method . A comparative study of inhibition values of
... Show MoreThe compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy
... Show MoreIn the present study, metal complexes of Mn(II), Ni(II), Co(II), Cu(II) and Hg(II) were synthesized using new Tetraazamacrocyclic Schiff Base (5E,8E,14E,17E)-6,8,15,17-tetramethyl-1,2,3,4,4a,7,9a,10,11,12,13,13a,16,18a-tetradecahydrodibenzo [b,i][1,4,8,11]tetraazacyclotetradecine (L) derived from 1,2-diamino cyclo hexane with the acetyl acetone. Compounds have been exanimated and confirmed by fourier-transform infrared (FT-IR), ultraviolet-visible (UV-visible), proton nuclear magnetic resonance (1HNMR), carbon nuclear magnetic resonance (13CNMR), microelemental analyses (CHN), thermal analysis (TG), conductivity and magnetic susceptibility. The propose geometry for all complexes [MLCl2] structures were octahedral. Therm
... Show MoreAbstract
In this manuscript, a simple new method for the green synthesis of platinum nanoparticles (Pt NPs) utilizing F. carica Fig extract as reducing agent for antimicrobial activities was reported. Simultaneously, the microstructural and morphological features of the synthesized Pt NPs were thoroughly investigated. In particular, the attained Pt NPs exhibited spherical shape with diameter range of 5-30 nm and root mean square of 9.48 nm using Transmission Electron Microscopy (TEM) and Atomic Force Microscopy (AFM), respectively. Additionally, the final product (Pt NPs) was screened as antifungal and antibacterial agent against Candida and Aspergillus species as well as Gram-positive Staphyllococcus aureus and G
... Show MoreMetal-organic frameworks (MOFs) are a relatively new class of materials of unique porous structures and exceptional properties. Currently, more than 110,000 types of MOFs have been reported among the countless possibilities. In this study, we have synthesised a novel MOF using zirconium chloride as the metal source and 4,4'-dicarboxy-2,2'-biquinoline (bicinchoninic acid disodium salt) as the linker, which reacted in N,N-Dimethylformamide (DMF) solvent. Three preparation methods were employed to prepare five types of the MOF, and they were compared to optimize the synthesis conditions. The resulting MOFs, named Zr-BADS, were characterised using scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), microscopy, and
... Show MoreThis research aims to explain the effect of the imported inflation (which moves through the raise of global prices to Iraqi economy) over local prices, besides, the recognition the most important channels of imported inflation moving, its causes, effects, ways and policies that reduce the negative effects. To achieve the research aim, the deductive approach was adopted through using descriptive method to describe and determine phenomenon. The most important conclusion is that the research found out that there are two channels to transmission imported inflation in world. The first channel is the direct channel (prices) and the second channel is the indirect (income). The most important recommendation is to create sovereign fund (O
... Show MoreThe main function of a power system is to supply the customer load demands as economically as possible. Risk criterion is the probability of not meeting the load. This paper presents a methodology to assess probabilistic risk criteria of Al-Qudus plant before and after expansion; as this plant consists of ten generating units presently and the Ministry Of Electricity (MOE) is intending to compact four units to it in order to improve the performance of Iraqi power system especially at Baghdad region. The assessment is calculated by a program using Matlab programming language; version 7.6. Results show that the planned risk is (0.003095) that is (35 times) less than that in the present plant risk; (0.1091); which represents respectable imp
... Show MoreThis research was one of the terms that used by Al-Bazzar in his musnad and this term was (Al-azza) who launched on some ways and hadiths and I collected those narration, and I have graduated and studied it to access to the meaning which Al-Bazzar want that from this description. In the introduction of the research, I have mention the importance of the subject and the reasons for his selection and also my plan, a preface where I mentioned the definition of Al-Bazzar and his musnad, then in the first section I defined Al-azza linguistically and idiomatically , the second section I studied the hadiths that Al-Bazzar described them with azza ,and then I conclude it with my results that I have reach
... Show MoreThe effects of scattering and secondary radiation generated inside the material on dose equivalent rate where studied using Co60 and Cs137 sources of activity (199.8 , 177.6) MBq , respectively for different thicknesses of Al , Pb and Pb- glass . The results showed that the equivalent rate increases when the effect of scattering was included for Al and Pb shields with cobalt-60 source of energy 1.25 MeV ; and decreases for Pb shield with Cs-137 source of energy 0.662MeV .The results showed also that the atomic number of The material effects the dose equivalent rate . The Pb-glass shield was found to be more efficient in absorption than other shields.