The aim of this study was to explain why 5-ethyldeoxyuridine (EUdR) showed cytotoxic activity against Ehrlich ascites tumour (EAT) cells in vitro but not in vivo. In vitro studies showed that EUdR was phosphorylated to nucleotides which inhibit thymidylate synthetase and DNA polymerase. Toxicity...

The synthesis of 5-ethyl-2′-deoxyuridine-5-monophosphate (EtdUrdMP) and an improved method for the purification of deoxythymidylate synthetase (TdRMP synthetase) from E. coli are described. TdRMP synthetase was inhibited competitively by EtdUrdMP (K1 = 2·2 × 10−5 M). Under similar conditions ...

The major metabolite of 5-ethyl-2′-deoxyuridine in rats has been isolated and purified by preparative thick layer and column chromatography. By mass and 1H NMR spectroscopy, it was identified as 5-(1-hydroxyethyl) uracil; the structure was confirmed by comparison with an authentic sample.

In the rat, the highly potent anti-herpes drug (E)-5-(2-bromovinyl)-2′-deoxyuridine (BVdUrd) is rapidly converted to its base (E)-5-(2-bromovinyl)uracil (BVUra) through the action of pyrimidine nucleoside phosphorylases. However, BVdUrd can be regenerated or even generated de novo from BVUra by...

The thermal and nuclease stabilities of G-quadruplexes consisting of oligodeoxynucleotides (ODNs) containing 5-[N-[2-[N,N-bis(2-aminoethyl)amino]ethyl]carbamoyl]-2′-deoxyuridine (BAE) or 5-[N-[3-[N,N-bis(3-aminopropyl)amino]propyl]carbamoyl]-2′-deoxyuridine (BAP) are described. We found that t...

The reaction of [14C]CO2, generated from [14C]BaCO3, with ethynylmagnesium bromide (5) at −78°C afforded [14C]propiolic acid (6). Methylation of [14C]propiolic acid and condensation of the resulting [14C]methyl propiolate (7) with the oxazoline (3) afforded [4-14C]2,2′-anhydrouridine (8) in 27...

Diastereomers of 5-ethyl-5-halo-6-methoxy-5,6-dihydro-2′-deoxyuridine were synthesized by the regiospecific addition of XOMe (X = Br, Cl) to the 5,6-olefinic bond of 5-ethyl-2′-deoxyuridine (EDU). 5-(1-Hydroxyethyl)-2′-deoxyuridine (HEDU) was identified as a metabolite of the 5-bromo-5-ethyl-...

Herpes simplex virus thymidine kinase type 1 (HSV1-TK) is frequently used as reporter protein in gene therapy. Our aim is to produce single photon emitting reporter probe based on technetium-99m. The synthesis of organometallic technetium and rhenium complexes of a 5′-carboxamide 5-ethyl-2′-de...

Pharmacokinetic parameters for 5-ethyl-2′-deoxyuridine (EDU) were determined following intravenous (iv) and oral (po) dosing in male Balb-C mice and iv dosing in male Sprague-Dawley rats. The concentrations of EDU in blood after 100 mg/kg iv bolus injections into mice and rats were consistent w...

Fosmidomycin is a natural antibiotic with promising IspC (DXR, 1-deoxy-d-xylulose-5-phosphate reductoisomerase) inhibitory activity. This enzyme catalyzes the first committed step of the non-mevalonate isoprenoid biosynthesis pathway, which is essential in Plasmodium falciparum and Mycobacterium...

It has been repirted that nandrolone decanoate is helpful in overcoming the neutropenic phase following irradiation. In the present study the influence of nandrolone decanoate on the thymus' cellularity after total body irradiation was investigated. In comparison with a placebo-treated grou...

A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that...

2-Methyl-1,2-oxaphospholan-5-one 2-oxide (OP) is useful in a wide range of flame-retarded compositions. It is a thermally stable substance which, in inert atmosphere, looses weight at 200 °C on dynamic heating, leaving a solid residue, the amount of which is sensitive to the presence of moistur...

Electrode reaction of bis(acetylacetonato)platinum(II), Pt(acac)2, and preparation of platinum (Pt) nanoparticles have been studied in 1-R-1-methylpyrrolidinium bis(trifluoromethylsulfonyl)amide (R = butyl, hexyl and decyl, which are abbreviated as BMPTFSA, HMPTFSA and DMPTFSA, respectively) ion...

The behaviour of three organic ligands in suspensions of fresh and degraded hydrated ordinary Portland cement pastes (HCP) has been investigated. EDTA arises as a decontamination product whilst ISA (isosaccharinic acid) is a main degradation product of cellulose. GLU (gluconic acid) is used as a...

Selenium and copper nanoparticles exhibit superior antioxidant activity, unique properties, and great potential applications that make them very attractive for developing new composite materials. In this study, polyethersulfone (PES) ultrafiltration membrane was modified by dispersing nano-sized...

Nixtamalised flour from transgenic maize (genetically modified maize with the cDNA of amarantin) and its tortillas were evaluated for some technological and nutritional properties and compared to the commercial brand MASECA™. Nixtamalised transgenic maize flour (NTMF) showed higher protein conte...

The potential use of quality protein transgenic maize (genetically modified maize with the cDNA of amarantin) for preparation of flour and tortillas through an extrusion lime cooking process was investigated. Tortillas from extruded transgenic maize flour had similar physicochemical and sensory ...

Herein, we describe short and efficient syntheses of isoxazole-3-carboxylic acid 3a and imino-oxopentanoic acid 8 achiral precursors of 4-hydroxyisoleucine. The developed procedures involve readily available and cheap starting materials and can easily be transposed to the large scale.

In the past decades, complex hydrides and complex hydrides-based materials have been thoroughly investigated as materials for energy storage, owing to their very high gravimetric and volumetric hydrogen capacities and interesting cation and hydrogen diffusion properties. Concerning hydrogen stor...