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.
The preparation and characterization of the Cu (II), Co(II), Ni(II), Zn(II), Cd(II), and Hg(II) metal complexes of heterocyclic azo ligand 2-[(4`-sulphamide phenyl) azo] -4,5-diphenyl imidazole (4-SuBAI) have been studied by elemental analysis, FT-IR and UV-Vis Spectroscopic, magnetic moment and molar conductance methods. The analytical data showed that all chelate complexes were prepared with (metal-ligand) ratio of (1:2). The general formula of these complexes was [ML2X2]. nH2O [were L=2-[(4`-sulphamide phenyl) azo]-4,5-diphenyl imidazole and X=Cl, and the octahedral geometry were suggested for these complexes .
In this work, polyvinylpyrrolidone (PVP), Multi-walled carbon nanotubes (MWCNTs) nanocomposite was prepared and hybrid with Graphene (Gr) by casting method. The morphological and optical properties were investigated. Fourier Transformer-Infrared (FT-IR) indicates the presence of primary distinctive peaks belonging to vibration groups that describe the prepared samples. Scanning Electron Microscopy (SEM) images showed a uniform dispersion of graphene within the PVP-MWCNT nanocomposite. The results of the optical study show decrease in the energy gap with increasing MWCNT and graphene concentration. The absorption coefficient spectra indicate the presence of two absorption peaks at 282 and 287 nm attributed to the π-π* electronic tr
... Show MoreThis paper studies the main characteristics of the traditional urban configuration of Arab cities, as an important built heritage, discussing the approach adopted with such configuration at the local level, and examines its ability to preserve the character of the city, as well as, its responsiveness to the recent requirements of its society that constantly change; in order to reach the appropriate procedures to deal with the traditional urban configuration of the Iraqi city to achieve a vital cultural communication with the vernacular built heritage, by dealing with the Form-Moral Values structure. Due to its importance within other traditional Iraqi cities, the research chose Al-Kadhimiya as a case study, so it discusses and compares
... Show MoreFolic acid modulates several disorders in humans, pregnancy mostly because of the mitochondria-rich placenta, is a condition that favors oxidative stress.Transitional metals, especially iron, which are particularly abundant in the placenta, are important in the production of free radicals. Adenosine deaminase (ADA), an enzyme essential for the differentiation of lymphoid cells, has been used for monitoring diseases with altered immunity. In the present study we investigated the effect of regular and irregular administered folic acid in the first and second trimester of pregnancy to be compared with non-pregnant women ,and also the effect of regular and irregular using of folic acid supplement on oxidative stress parameters an
... Show MoreDiabetes mellitus can be defined as a metabolic disorder disease .Complication of diabetes are due to diabetic nephropathy .This study was done in vitro to study the effect of different concentrations of erlotinib inhibitor ( tyrosine kinase inhibitor) on electrolyte levels (MgâºÂ²,CaâºÂ²,Naâº) in sera of Iraqi patients with newly diagnosis type2 diabetes and diabetic nephropathy in addition to find the best percentage inhibition for utilizing different concentrations from erlotinib (6.97x10â»â·, 9.30x10â»â· ,1.16x10â»â¶,1.39x10â»â¶ ,1.62x10â»âµ )molar on electrolyte levels . This study was conducted in The National Diabetes Ce
... 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 MoreA series of new coumarin and N-amino-2-quinolone derivatives have been synthesized. The reaction of coumarin (1) with excess of Hydrazine hydrate 98% yielded 1-amino-2-quinolone (2), Compound (2) was reacted with different Sulfonyl chloride to yield Sulfonamides [ N-(2-oxoquinolin-1(2H)-yl) methane sulfonamide (3), N-(2-oxoquinolin-1(2H)-yl) Benzene sulfonamide (4) and 4-methyl-N-(2-oxoquinolin-1(2H)-yl) benzene sulfonamide (5) ], while reaction of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetic acid (8) with different amines yielded compounds [ 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(2-oxoquinolin-1(2H)-yl) acetamide (9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamide (10) ] th
... Show MoreSchiff bases, named after Hugo Schiff, are aldehyde- or ketone-like compounds in which the carbonyl group is replaced by imine or azomethine group. They are widely used for industrial purposes and also have a broad range of applications as antioxidants. An overview of antioxidant applications of Schiff bases and their complexes is discussed in this review. A brief history of the synthesis and reactivity of Schiff bases and their complexes is presented. Factors of antioxidants are illustrated and discussed. Copyright © 2016 John Wiley & Sons, Ltd.
1,3,4-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
Nearly a century and a half has passed since Sarah Orne Jewett published her much anthologized short story “A White Heron” (1886), but commentators on the tale missed one of the most important points in the text. It is the story’s similarity to the traditional Euro-centric fairy tale of “Little Red Riding Hood”. As an author, writing at the end of the ninetieth century, a time that witnessed the demise of the Romantic movement in America and the beginning of the age of Realism, Jewett did not romanticize her characters, despite the idyllic landscape in which “A White Heron” is set. Her story can be analyzed as a text that aims at disseminating ecological awareness among her young readers. This study focuses on Jewett
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