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.
This paper presents L1-adaptive controller for controlling uncertain parameters and time-varying unknown parameters to control the position of a DC servomotor. For the purpose of comparison, the effectiveness of L1-adaptive controller for position control of studied servomotor has been examined and compared with another adaptive controller; Model Reference Adaptive Controller (MRAC). Robustness of both L1-adaptive controller and model reference adaptive controller to different input reference signals and different structures of uncertainty were studied. Three different types of input signals are taken into account; ramp, step and sinusoidal. The L1-adaptive controller ensured uniformly bounded
... Show MoreHygienic engineering has dedicated a lot of time and energy to studying water filtration because of how important it is to human health. Thorough familiarity with the filtration process is essential for the design engineer to keep up with and profit from advances in filtering technology and equipment as the properties of raw water continue to change. Because it removes sediment, chemicals, odors, and microbes, filtration is an integral part of the water purification process. The most popular technique for treating surface water for municipal water supply is considered fast sand filtration, which can be achieved using either gravity or pressure sand filters. Predicting the performance of units in water treatment plants is
... Show MoreHygienic engineering has dedicated a lot of time and energy to studying water filtration because of how important it is to human health. Thorough familiarity with the filtration process is essential for the design engineer to keep up with and profit from advances in filtering technology and equipment as the properties of raw water continue to change. Because it removes sediment, chemicals, odors, and microbes, filtration is an integral part of the water purification process. The most popular technique for treating surface water for municipal water supply is considered fast sand filtration, which can be achieved using either gravity or pressure sand filters. Predicting the performance of units in water treatment plants is a basic pri
... Show MoreA new Macrocyclic Schiff base ligand Bis[4-hydroxy(1,2-ethylene-dioxidebenzylidene) pheylenediamine] [H2L] and its complexes with (Co(II) , Ni(II) , Cu(II) , Zn(II) and Cd(II)) are reported . The ligand was prepared in two steps,in the first step a solution of (o-phenylene diamine) in methanol react under reflux with (2,4-dihydroxybenzylaldeyed) to give an (intermediatecompound) [Bis-1,2 (2,4-dihydroxybenzylediene)pheylinediamine] which react in the second step with (1,2- dichloro ethane) giving the mentioned ligand.Then the complexes were synthesis of adding of corresponding metal salts to the solution of the ligand in methanol under reflux with 1:1 metal to ligand ratio. On the basis of, molar conductance, I.R., UV-Vis, chloride content a
... Show MoreIn this work, prepared new ligand namely 5-(2,4-dichloro-phenyl)-1,3,4-oxadiazole-2-(3H)-thion, was obtained from the 2,4-dichlorobenzoyl chloride with hydrazine, after that reaxtion with CS2/KOH in methanol.
في هذا البحث تم تحضير المركبات المعدنية النانوية الجديدة لأيونات البلاتين 4+و الذهب 3+ مع ليكاند قاعدة مانخ جديد مشتق من السيبروفلوكساسين بطريقة الموجات فوق الصوتية. تم تشخيص المعقدات النانوية والليكاند الجديد بأستخدام تقنيات فيزيائية و كيميائية مختلفة مثل أطياف الاشعة تحت الحمراء، حيود الاشعة السينية ، المجهر الالكتروني الماسح ، المجهر الالكتروني النافذ و مجهر القوة الذرية. تم تحديد نشاط مضادات الأك
... Show MoreIn the present study, mixed ligand compounds of Mn(II), Ni(II), Co(II), Cu(II), Cd(II) and Hg(II) were synthesized using new Ligand N1,N4-bis (pyrimidin-2-ylcarbamothioyl) succinimide (NPS) derived from [Butanedioyl diisothiocyanate with 2- aminipyridine] as first ligand, proline (pro) as second ligand and evaluation of their antioxidant activities for ligand, nickel and cobalt complex towards 1.1-Di-phenyl-2picrylhydrazyl (DPPH) will be compared to the standard anti-oxidants (i.e. the ascorbic acid). Those materials that have been prepared provided results are a result of exhibiting different activities of the radical scavenging for all of the compounds. Compounds were observed then confirmed through the Fourier-tra
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for t
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