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 research aimed to know favoured mass media for children and
modifying their behaviour ,the child became aquires the information from
mass media that he exposure them without any guidance , where upon the
quidance proqrammes becomes real danger whereas qet out their civil
style and converting to deadly poisons,and because of little study for this
supject the two researchers opined to perform astudy to know the favoured
mass media to the children and what are the mass media that modify their
behavior according to ther parent points of view ,after propring the research
measurement and the suilable statical methods it has shown that there are
mass media affect in children behavior ,they are st
ABSTRACT
The study aimed to evaluate the information label of some local pickle products and estimate sodium benzoate therein. 85 samples of locally made pickles were collected from Baghdad city markets and randomly from five different areas in Baghdad it included (Al-Shula, Al-Bayaa, Al-Nahrawan, Al-Taji, and Abu Ghraib), which were divided into groups P1, P2, P3, P4 and P5, respectively, according to those areas, samples information label was scanned and compared with the Iraqi standard specification for the information card of packaged and canned food IQS 230, the results showed that 25.9% of the samples were devoid of the indication card informa
... Show MoreThe research aims to apply the novel forward osmosis (FO) process to recover pure water
from contaminated water. Phenol was used as organic substance in the feed solution, while sodium
chloride salt was used as draw solution. Membranes used in the FO process is the cellulose
triacetate (CTA) and polyamide (thin film composite (TFC)) membrane. Reverse osmosis process
was used to treatment the draw solution, the exterior from the forward osmosis process. In the FO
process the active layer of the membrane faces the feed solution and the porous support layer faces
the draw solution and this will show the effect of dilutive internal concentration polarization and
concentrative external concentration polarization.
In th
The aim of the research is to identify the international accounting standards and accounting standards for Islamic banks, and to analyze the most important problems in the application of Islamic accounting standards, as well as to analyze some of the principles and methods used in the application of accounting standards in Islamic banks. The research was built on three hypotheses, the first being (there is a tangible impact on the application of international accounting standards for banks’ management of liquidity, achieving profits, maintaining property rights and fulfilling their obligations), and the second (the bank facing obstacles using Islamic accounting standards, as it is expected that when using Islamic accounting standar
... Show MoreFuture generations of wireless networks are expected to heavily rely on unmanned aerial vehicles (UAVs). UAV networks have extraordinary features like high mobility, frequent topology change, tolerance to link failure, and extending the coverage area by adding external UAVs. UAV network provides several advantages for civilian, commercial, search and rescue applications. A realistic mobility model must be used to assess the dependability and effectiveness of UAV protocols and algorithms. In this research paper, the performance of the Gauss Markov (GM) and Random Waypoint (RWP) mobility models in multi-UAV networks for a search and rescue scenario is analyzed and evaluated. Additionally, the two mobility models GM and RWP are descr
... Show Moreلقد كان حرص المؤلف على إصدار هذا الكتاب نابعا ً من قناعة تامة بأن مجال التقويم والقياس بحاجة إلى كتاب علمي حديث يتناول عرض أدوات الاختبار والقياس والمتمثلة بالصدق والثبات ويتسم بالوضوح في التعبير عن المفاهيم والمصطلحات والأنواع لكل منها ليكون وسيلة مبسطة بأيدي الأساتذة والباحثين وطلبتي الدراسات العليا الماجستير والدكتوراه لإستخراج صدق وثبات الاختبارات والمقاييس بطرق إحصائية متقدمة من خلال إستخدام البرنا
... Show MoreBasketball is a popular game in many parts of the world and many developed countries are making continuous efforts to prepare and develop their emerging players on scientific and clear bases as the basis for reaching high levels The researchers used the descriptive approach in the method of correlative studies to suit the nature of the study The readymade software (IBM SPSS Statistics Version24) was used to perform statistical treatments The researchers concluded that there was a significant relationship between body size indicators (height and weight) with the fitness elements of the emerging basketball players The researchers recommended conducting a similar study to determine the type of relationship to the indicators of the physical str
... Show MoreA biconical antenna has been developed for ultra-wideband sensing. A wide impedance bandwidth of around 115% at bandwidth 3.73-14 GHz is achieved which shows that the proposed antenna exhibits a fairly sensitive sensor for microwave medical imaging applications. The sensor and instrumentation is used together with an improved version of delay and sum image reconstruction algorithm on both fatty and glandular breast phantoms. The relatively new imaging set-up provides robust reconstruction of complex permittivity profiles especially in glandular phantoms, producing results that are well matched to the geometries and composition of the tissues. Respectively, the signal-to-clutter and the signal-to-mean ratios of the improved method are consis
... Show More