5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds. ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed enhanced cytotoxic effects for [IV] over 5-FU.
New derivatives of Schiff bases were synthesized from the aldehyde derivative (Ma2) which was produced by reacting the mefenamic acid (Ma) with thionyl chloride to obtain the acid halide derivative (Ma1). Compound (Ma1) was dissolved in DMF and mixed with p-hydroxybenzaldehyde which was previously dissolved with pyridine to obtain the aldehyde derivative (Ma2). In the final step, derivatives of Schiff bases were synthesized by reacting the aldehyde (Ma2) with a number of different aromatic primary amines in the presence of glacial acetic acid to obtain the new derivatives Ma [3-10]. The new prepared compounds were characterized by melting points and with spectral data FT-IR, 13C-NMR and 1H-MNR (some of them). The vital effectiven
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
Background: A great dental and biomedical interest had been paid to silver nanoparticles because of their antimicrobial activity. Objective: To evaluate the antimicrobial and cytotoxic activity of a newly developed Nano-silver fluoride that was synthesized from moringa oleifera leaf extract against S. mutants. Material and method: The green synthesis method was used to prepare Nano-silver fluoride from moringa oleifera leaf extract. The minimum inhibitory concentration and the minimum bactericidal concentration were evaluated using brain heart infusion plates, while the cytotoxicity was evaluated by the hemolytic activity. Results: Nano-silver fluoride had a bactericidal and bacteriostatic effect (MIC was 60 ppm and MBC was 120 pp
... Show MoreThe research deals with metaphors as being one of the primary means used by Lyudmila Ulitskaya when writing the novel " Sincerely Yours Shurik ", to form diverse and multifaceted collective female images of representatives of the classic psychological patterns presented in the work. This research reflects the results of the study related to the work of Lyudmila Yevkinevna Ulitskaya, an actress of modern Russian prose. The novel "The Sincerely to You Shorek" is one of Ludmila Ulitskaya's creations (the year of writing - 2003), which, like her other works, is distinguished by a unique presentation style, rich vocabulary, lexical and semantic diversity, and a special style of writing. writer. The main objective of the research is to look at th
... Show Moreالوصف A simple chemistry method approach was used to synthesise new ligand derivate from L-ascorbic acid and its complexes. All of them were water-soluble and are used quite extensively in the medical and pharmaceutical fields. This study synthesised the new ligand derivative from L-ascorbic acid-base using the following steps: A 5, 6-O-isopropylidene-L-ascorbic acid was prepared by reacting dry acetone with L-ascorbic acid followed by reacting it with trichloroacetic acid to yield [chloro (carboxylic) methylidene]-5, 6-O-isopropylidene-L-ascorbic acid in the second stage. In the third stage, the derivative was reacted with (methyl (6-methyl-2-pyridylmethyl) amine to create a new ligand (ONMILA). This novel ligand was identified using
... Show MoreContemporary life is racing against time in its temptations and variables, and it has become shaped and changed in an amazing way in its various aspects and fields. This was facilitated by intellectual and scientific communication between civilizations, and the rapid progression in successive inventions and discoveries in the fields of science and arts of knowledge. This contributed to a great economic and commercial renaissance. Then, these economic developments entered the world into a very strong competition, which forced producers to calculate all production costs, to reach the highest profits by reducing the price of the produced commodity on the one hand, and achieving quality in appearance (especially) on the other hand. Since the ma
... Show MoreMaximizing the net present value (NPV) of oil field development is heavily dependent on optimizing well placement. The traditional approach entails the use of expert intuition to design well configurations and locations, followed by economic analysis and reservoir simulation to determine the most effective plan. However, this approach often proves inadequate due to the complexity and nonlinearity of reservoirs. In recent years, computational techniques have been developed to optimize well placement by defining decision variables (such as well coordinates), objective functions (such as NPV or cumulative oil production), and constraints. This paper presents a study on the use of genetic algorithms for well placement optimization, a ty
... Show MoreIn this research a new compounds were synthesized started from compound 1 which was synthesized from two moll of piperidine (secondary cyclic amine) with dichloro acetic acid, compound 1 reacted by condensation reaction with methanol and H 2 SO 4 as a catalyst to give the ester compound 2. Compound 2 was reacted with hydrazine hydrate 80 % to give compound 3 , then the compounds 4-13 were synthesized from refluxing of compound 3 with the selected aldehydes and ketones via using few drops of glacial acetic acid, finely step the compounds 4-13 were reacted with phtalic anhydride to give compounds 14-23.. All these compounds were characterized by using of melting point, FTIR, 1 HNMR and mass spectroscopy. Scheme 1 and Scheme 2 shown the all re
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