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 search involve the synthesis of some new 1,3-oxazepine and 1,3-diazepine derivatives were synthesized from Schiff base. The Schiff base (VIII) prepared from reaction of aldehyde (IV) derived from L-ascorbic acid with aromatic amine ([2-(4- nitrophenyl)-5-(4-aminophenyl)-1,3,4-oxadiazole] (VII). Oxazepine compounds (IX-XI) were synthesized from the cyclic condensation of Schiff base (VIII) with (maleic, phthalic and 3-nitrophthalic) anhydride, compounds (IX-XI) that were reacted with p-methoxyaniline to give diazepine derivatives (XII-XIV). The structures of the new synthesized compounds have been confirmed by physical properties and spectroscopy measurements such as FTIR, and some of them by 1 H-NMR, 13 CNMR, Mass, and evaluated
... Show MoreA new Schiff base ligand was prepared via a condensation reaction. The synthesis involved combining N-(4-aminophenylsulfonyl) benzamide (also known as sulfabenzamide) with indoline-2,3-dione. To facilitate the reaction, three drops of glacial acetic acid were added. This process yielded the ligand N-(4-(2-oxoindoline-3-ylideneamino) phenylsulfonyl) benzamide, designated as (L). Mixed ligand complexes were prepared in a molar ratio (1:1:1) (M:1,10-phen, L) at concentrations of 10-4M by interacting L and 1,10-phenanthroline, with the following metal ions (Cr+3, Mn+2, Zn+2, Pd+2, Cd+2, Pt+4). These complexes exhibited different geometric shapes, including (octahedral for both Cr+3, Mn+2, Pt+4, tetrahedral for Zn+2 and Cd+2, an
... Show MoreMany designs have been suggested for unipolar magnetic lenses based on changing the width of the inner bore and fixing the other geometrical parameters of the lens to improve the performance of unipolar magnetic lenses. The investigation of a study of each design included the calculation of its axial magnetic field the magnetization of the lens in addition to the magnetic flux density using the Finite Element Method (FEM) the Magnetic Electron Lenses Operation (MELOP) program version 1 at three different values of current density (6,4,2 A/mm2). As a result, the clearest values and behaviors were obtained at current density (2 A/mm2). it was found that the best magnetizing properties, the high
... Show MoreReservoir characterization is an important component of hydrocarbon exploration and production, which requires the integration of different disciplines for accurate subsurface modeling. This comprehensive research paper delves into the complex interplay of rock materials, rock formation techniques, and geological modeling techniques for improving reservoir quality. The research plays an important role dominated by petrophysical factors such as porosity, shale volume, water content, and permeability—as important indicators of reservoir properties, fluid behavior, and hydrocarbon potential. It examines various rock cataloging techniques, focusing on rock aggregation techniques and self-organizing maps (SOMs) to identify specific and
... Show MoreComplexes of Au(III) ,Pd (II) , Pt (IV ) and Rh(III) with S – propynyle -2- thiobenzimidazole (BENZA) have been prepared and characterized by IR and UV- Visible spectral methods in addition to magnetic and conductivity measurements and micro – elemental analysis (CHN).The probable structures of the new complexes have been suggested.
في هذا البحث تم تحضير المركبات المعدنية الجديدة لأيونات البلاتين (الرباعي) و الذهب (الثلاثي) مع ليكاند قاعدة مانخ جديد مشتق من السيبروفلوكساسين . تم استخدام المعقدات بعد ذلك كمصدر لتحضير جزيئات عن طريق ترسيب المعقدات على مسام دقائق السيليكا النانوية. Si/Au2O3 Si/PtO2 تم تشخيص الليكاند و معقداته
... Show MoreA multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (
Methotrexate (MTX), a folic acid antagonist is widely used for the treatment of a variety of tumors. In the present study, the possible protective effect of aqueous green tea extract (AGTE) in methotrexate-induced haematotoxicity was investigated.Four main groups of white Albino rats were used: control group, (MTX) group, following a single dose of MTX (20 mg/kg, i.p.) saline was administered for 5 days. (AGTE) group, was treated with 1.25% concentration of AGTE only for 12 days and the (MTX+AGTE) group, in thism group rats received different concentrations of AGTE (0.625, 1.25 and 2.5%), as their sole source of drinking water, 7days before and 5 days after MTX treatment. MTX induced significant decreases in RBC, Hb, Hct, WBC and pl
... Show Moreنظرة عامة: تُعرَّف المادة أو العامل الذي يمكن أن يؤثر على الحمض النووي أو الكروموسومات على أنه سم جيني. قد يؤدي تلف الحمض النووي في الخلية الجسدية إلى حدوث طفرة جسدية ، والتي قد تحفز التحول الخبيث ، في حين أن الضرر الذي يلحق بالخلية الجرثومية قد يؤدي إلى تغيير خاصية وراثية (طفرة في السلالة الجرثومية) (سرطان). أحد الأحماض الدهنية الأحادية غير المشبعة الأحادية غير الأساسية هو حمض البالميتوليك. بعد حمض الأوليك
... Show MoreThe purpose of this study is to underline the progression and development of research regarding oxygen-containing heterocycles as well as the contribution that some oxygen-containing heterocycles have made as anticancer medicines. A series of publications about the antitumor effects of derivatives of heterocyclic compounds containing an oxygen atom, such as furan, benzofuran, oxazole, benzoxazole, and oxadiazole, were evaluated, and their anticancer activities showed encouraging results when compared to those of established standard treatments.