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.
The reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.
Q-switch Nd: YAG laser of wavelengths 235nm and 1,460nm with energy in the range 0.2 J to 1J and 1Hz repetition rate was employed to synthesis Ag/Au (core/shell) nanoparticles (NPs) using pulse laser ablation in water. In this synthesis, initially the silver nano-colloid prepared via ablation target, this ablation related to Au target at various energies to creat Ag/Au NPs. Surface Plasmon Resonance (SPR), surface morphology and average particle size identified employing: UV-visible spectrophotometer, scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The absorbance spectra of Ag NPs and Ag/Au NPs showed sharp and single peaks around 400nm and 410nm, respec
The target of this study was to synthesize several new Ciprofloxacin drug analogs by providing a nucleophilic substitution procedure that provides new functionality at the carboxylic group location. The analogs were synthesized, designed, and characterized by 1HNMR, and FTIR. The synthetic path began from the reaction of ciprofloxacin drug with morpholine to give compound[B], ciprofloxacin derivative was linked with a variety of primary and secondary amines to give compounds[B1-B9]. The above-mentioned prepared compounds [B3 and B5] were applied to liver enzymes, and the increase in the activity of these enzymes was observed. In addition, a theoretical study was conducted to study the energies and properties of the prepared co
... Show MoreThe study involved preparing a new compound by combining Schiff bases generated from compounds for antipyrine, including lanthanide ions (lanthanum, neodymium, erbium, gadolinium, and dysprosium). The preparation of the ligand from condensation reactions (4-antipyrinecarboxaldehyde with ethylene di-amine) at room temperature, and was characterization using spectroscopic and analytical studies ( FT-IR, UV-visible spectra, 1H-NMR, mass spectrometry, (C.H.N.O), thermogravimetric analysis (TGA), in addition to the magnetic susceptibility and conductivity measurement of the synthesis complexes, among the results we obtained from the tests, we showed that the ligand behaves with the (triple Valence) lanthanide ions, the multidentate
... Show MoreThe research dealt with the topic ' the aesthetics of design shape of interior spaces for the syndicate of physicians' as it reflects visions evolving to the level of tasting and positive interpretation for the space of work to be on a high design level.The research consisting of four chapters as follow; The first chapter examined the problem of the research contracted in the following question: Have the design shapes any role in achieving and showing the aesthetic side for the syndicate of physicians? so the goal of the research was showing the aesthetics of design shape of interior spaces for the syndicate of physicians, The chapter also included the objective spatial and temporal limits of research .Finally the terms were specified. T
... Show MoreThis paper describes a new proposed structure of the Proportional Integral Derivative (PID) controller based on modified Elman neural network for the DC-DC buck converter system which is used in battery operation of the portable devices. The Dolphin Echolocation Optimization (DEO) algorithm is considered as a perfect on-line tuning technique therefore, it was used for tuning and obtaining the parameters of the modified Elman neural-PID controller to avoid the local minimum problem during learning the proposed controller. Simulation results show that the best weight parameters of the proposed controller, which are taken from the DEO, lead to find the best action and unsaturated state that will stabilize the Buck converter system performan
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