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.
Abstract
The objective of this research is to analyze the relationship between the strategic planning for human resources and career path, and I have tested Search the Ministry of Health and some health centers headquarters in the Karkh district, that is applied in sample Consist of (45) Deputy Director, Head of Depts, Departmental Manager, and health center Manager.
Find interested in studying the two subjects are important and vital, at the level of organizations at the present time, namely the strategic planning of human resources and career path. To achieve the objectives of the research was designed Qusestionnair (31) items to collect Primary data. and collected t
... Show MoreFor a long time, the intensification of profit represented a major goal for the company management ,but this goal confirmed a series of restrictions such the constriction on short period, the time rather than on long and medium strategic goal, the relationships with customers ,the supplies, employees , This goal is replaced by another one (intensification of the company's value) ,and the fortune of the share holders itself ,for the purpose of creating value, the company must generate great outcomes to cover the operating expense and to insure the a suitable compensation to the invested capital (the market value added) is the indication used to estimate the company ability to create value –added the development
... Show MoreBrick factories distributed within the study area use fuel oil to complete the burning of the bricks, were high amounts of gases and suspended particles with different concentrations of heavy elements are produced and cause air and soil pollution. It is noted that the workers suffer from respiratory diseases and other health problems. This study is an attempt to detect the sources and concentrations of pollutants and to propose modalities for their treatment and reduction. Air and soil samples were collected from different sites in Abu Smeache brick factory in Al-Kifl area to the south of Babel city, Iraq, during two seasons (summer and winter). The process also included collecting and modelling of dust and soil
... Show MoreSoil resistivity depends on many overlapping factors, which influence it in various ways. The aim of this study was to determine the effects of some physical and chemical factors on soil apparent resistivity. The results of field, laboratory, and statistical studies revealed a complex relationship between water content, pH, and salinity with soil apparent resistivity. The results showed that water content had a clear effect on apparent resistivity, as it increased significantly when water content value decreased to less than about 5%. The results also showed that increasing the salinity ratio at the expense of water content led to an increase in the apparent resistivity values. The apparent resistivity values also increased significantly
... Show MorePoly-ether-ether-ketone (PEEK) was introduced in dentistry as an alternative to metal alloys.
To assess the effectiveness of PEEK-fixed retainers in preserving the stability of mandibular anterior and participant satisfaction as compared to the Dead-soft coaxial fixed retainer (DSC).
A single-centre, two-arm parallel groups
The genus Serrasentis is one of important acanthocephalan parasites, parasitizing fish, birds and other vertebrates. Twenty two out of 500 fish specimens (4.4%) were found to be naturally infected with adult and cyst of worms of Serrasentis sp. which were collected from the stomach and intestine of Synaptura orientalis; Johnius belangrii, Otolithus ruber and Upeneus sulphureus fish species', from locations of Khor Abdullah, Arabian Gulf, Iraqi marine waters (29°58,33, N48°28, 20E) during the year 2017.The light and SEM study revealed that the adult worm have elongated and cylindrical body, anterior extremity with hooks forming combs arranged on the ven
... Show MoreThe Bouguer gravity and magnetic RTP data were used to detect the depth of basement rocks in middle and south Diyala Province, east Iraq. The depth of the basement rocks was calculated by using the Source Parameter Imaging (SPI) method. New attempt is achieved to applied the SPI technique to the gravity values to estimate the depth of basement rocks. The depths of basement map derived from gravity data range 8-14 km, the depth of basement map derived from magnetic data range 9-13.5 km and the basement depth prepared by C.G.G, 1974 range 9-11 km. The derived maps from SPI method and that prepared by C.G.G, 1974 show good matching in the distribution of the depths of the study area. This study showed that basement’s depth range from
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