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.
A novel series of mixed-ligand complexes of the type, [ML 1 (L 2 ) 3 ]Cl x [M = Cr(III), Fe(III), Co(II),Ni(II), Cu(II), Cd(II) and Hg(II), n = 2, 3], was synthesized using Schiffbase (HL 1 ) as main ligand, nicotinamide (L 2 ) as secondary ligand, and the corresponding metal ions in 1:3:1 molar ratio. The main ligand, HL 1 was prepared by the interaction of ampicillin drug and 4-chlorobenzophenone. The synthesized mixed ligand complexes were characterized by elemental analysis, UV-Vis, FT-IR, 1 H-NMR, 13 C-NMR and TG/DTG studies. In the mixed-ligand complexes, the Schiffbase ligand, HL 1 showed coordination to the central metal ion in tridentate manner via azomethine nitrogen, β-lactam ring oxygen and deprotonated carboxylic oxy- gen atom
... Show MoreThe five-a- Side Soccer for simple mental disability is as interesting and caring as many other sporting events. Therefore, the researchers believe that their basic skills tests are compatible with then level of the tested individuals in terms of age and mental ability. As a means of selecting those who are qualified to practice this game in a simple way, the problem of research has been identified in the design and standardization of two scoring skills that belong to this category and are approved by the training staff during the initial selection process. The research community is determined by people with mental disabilities who belong to the governmental and private institutes and the Special Olympics Union in Baghdad and for the year 2
... Show MoreIn this study, gold nanoparticles were synthesized in a single step biosynthetic method using aqueous leaves extract of thymus vulgaris L. It acts as a reducing and capping agent. The characterizations of nanoparticles were carried out using UV-Visible spectra, X-ray diffraction (XRD) and FTIR. The surface plasmon resonance of the as-prepared gold nanoparticles (GNPs) showed the surface plasmon resonance centered at 550[Formula: see text]nm. The XRD pattern showed that the strong four intense peaks indicated the crystalline nature and the face centered cubic structure of the gold nanoparticles. The average crystallite size of the AuNPs was 14.93[Formula: see text]nm. Field emission scanning electron microscope (FESEM) was used to s
... Show MoreTwo samples of (Ag NPs-zeolite) nanocomposite thin films have been prepared by easy hydrothermal method for 4 hours and 8 hours inside the hydrothermal autoclave at temperatures of 100°C. The two samples were used in a photoelectrochemical cell as a photocatalyst inside a cell consisting of three electrodes: the working electrode photoanode (AgNPs-zeolite), platinum as a cathode electrode, and Ag/AgCl as a reference electrode, to study the performance of AgNPs-zeolite under dark current and 473 nm laser light for water splitting. The results show the high performance of an eight-hour sample with high crystallinity compared with a four-hour sample as a reliable photocatalyst to generate hydrogen for renewable energies.
A new Schiff base ligand Bis-1,4-di[N-3-(2-hydroxy-1-amino)- acetophenonylidene] benzylidene [L] and its complexes with (Mn(II) ,Co(II) ,Ni(II and Cu(II)) were synthesized . The ligand was prepared in two steps. In the first step a solution of (terphthalaldehyde) in methanol reacts under reflux with (p-aminoacetophenone) to give an intermediate compound [1-[3-({4-[(3-Acetyl-phenylimino)-methyl]-benzylidene}-amino)-phenyl]- ethanone which reacts in the second step with (2-Amino-phenol) giving the mentioned ligand. The complexes were synthesized by addition the corresponding metal salt solution to the solution of the ligand in methanol under reflux in (1:1) metal to ligand ratio. On the basis of, molar conductance, I.R., UV-Vis, HPLC, chlorid
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