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.
NAA Mustafa, University of Sulaimani, Ms. c Thesis, 2010 - Cited by 4
The Mesopotamian soil is muddy and fertile, and so from ancient eras Iraqis used mud in their building, settlements and architecture in different methodologies according to the nature and the function of the building that was either in its pure form or by mixing it with other materials such as straw . also as raw bricks in different ways either for the whale building or parts of it, or for the finishing parts such as roofing for instance. In this research these different forms and methodologies will permeate through out a chosen examples of historical building, rural buildings and settlements and ancient buildings as well as some current uses of mud in the structures and building in standing cities, this in order to conclude some
... Show MoreThe formal integration of the interior spaces in general and the commercial spaces of the watch shops in the large commercial centers in particular is the goal that the designers aim to reach in order for the interior space to become successful in terms of the design idea and its characteristics. Implementation mechanism. One of the reasons for achieving formal integration in the interior spaces of watch shops is the requirements of the design that must be available in these spaces to reach a state of formal integration between the interior and the exterior so that the space becomes fully integrated in all respects. Because of the aforementioned reasons for dealing with the research, through four chapters: The first chapter included the
... Show MoreThe interior spaces represent a true reflection of the concepts and values of humanity and requirements; were interested in current research ongoing changes that have occurred in those human values and requirements over time, even pat each time warp its values and its own requirements. Those changes, which receive Bdilalha the spaces linked by a renewal which guarantees the interior design of the spaces of sustainability and bio-coordinated. Launched search from an initial perception that those associated with the changes of the spaces through time that have not been subject to examination and supervision, they will constitute a continuing threat of losing the ties with the past under the pretext of modernization and mo
... Show MoreZSM-5 zeolite was synthesis under hydrothermal conditions at 175oC. The synthesis parameters have been investigated to find optimum synthesis method. Firstly, the crystallization time has been investigated to find the optimum crystallization time. Also, the ageing time was studied. The morphology, structure, and composition of the synthesized ZSM-5 zeolite were characterized using scanning electron microscopy (SEM), pH meter, viscometer, and X-ray powder diffraction (XRD). The bulk Si/Al ratio of ZSM-5 zeolite was in the range of 9.5—11.7. The synthesized ZSM-5 zeolite with appropriate ageing time could adjust crystal size and degree of the crystallinity. The crystal size of ZSM-5 zeolite obtained at an agei
... Show MoreTitanium dioxide (TiO2) nanotubes have gained particular interest as a material for gas sensors because of their vertical arrays, prepared by the anodization procedure. The presence of several oxygen vacancies in these nanotubes facilitates gas diffusion and provides additional active sites. This study examined the impact of voltages on the process of depositing iron nanoparticles onto arrays of TiO2 nanotubes (TNTs) for use as a gas sensor. The TNTs are manufactured using a straightforward and economical electrochemical anodization technique, specifically for gas sensor applications. By varying the deposition voltage (2-6 volts), ordered Fe-TNTs were efficiently manufactured using a simple two-step electrochemical process. It utili
... Show MoreIn this investigation, water-soluble N-Acetyl Cysteine Capped-Cadmium Telluride QDs (NAC/CdTe nanocrystals), utilizing N-acetyl cysteine as a stabilizer, were prepared to assess their potential in differentiating between DNA extracted from pathogenic bacteria (e.g. Escherichia coli isolated from urine specimen) and intact DNA (extracted from blood of healthy individuals) for biomedical sensing prospective. Following the optical characterization of the synthesized QDs, the XRD analysis illustrated the construction of NAC-CdTe-QDs with a grain size of 7.1 nm. The prepared NAC-CdTe-QDs exhibited higher PL emission features at of 550 nm and UV-Vis absorption peak at 300 nm. Additionally, the energy gap quantified via PL and UV–Vis were 2.2 eV
... Show MoreIn this study, chemical oxidation was employed for the synthesis of polypyrrole (PPy) nanofiber. Furthermore, PPy has been subjected to treatment using nanoparticles of neodymium oxide (Nd2O3), which were produced and added in a certain ratio. The inquiry centered on the structural characteristics of the blend of polypyrrole and neodymium oxide after their combination. The investigation utilises X-ray diffraction (XRD), FTIR, and Field Emission Scanning Electron Microscopy (FE-SEM) for PPy, 10%, 30%, and 50% by volume of Nd2O3. According to the electrochemical tests, it has been noted that the nanocomposites exhibit a substantial amount of pseudocapacitive activity.