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At least 919 records · Page 51Linked to original sources
PubMed1975

Possible antineoplastic agents I.

A few thalidomide and glutarimide derivatives were synthesized. Several compounds possessed significant antineoplastic activity against Ehrlich ascites carcinoma in Swiss albino mice.

Animals↗
PubMed2005

Synthesis and evaluation of bifunctional nitrocatechol inhibitors of pig liver catechol-O-methyltransferase.

Bifunctional compounds were tested in vitro as potential inhibitors of pig liver catechol-O-methyltransferase (COMT) with respect to the catechol substrate 4-[(3,4-dihydroxyphenyl)azo]benzenesulfonate. The bifunctional compounds were a composite of either two nitrocatechols or one nitrocatechol and one phenol, linked by amide bonds to a spacer unit comprising two to five methylene groups. The unsymmetrical compounds N-[2-(4-hydroxybenzoylamine)ethyl]-3,4-dihydroxy-5-nitrobenzamide], N-[3-(4-hydroxybenzoyl-amine)propyl]-3,4-dihydroxy-5-nitrobenzamide] and N-[5-(4-hydroxybenzoylamine)pentyl]-3,4-dihydroxy-5-nitrobenzamide] demonstrated strong inhibitory action against COMT with K(i) values in the 100 nM range. In comparison, the monofunctional nitrocatechol analogues of these compounds had K(i) values that were significantly higher.

Animals↗
PubMed2004

Determination of mono-, di- and trinitronaphthalenes in soil samples contaminated by explosives.

We investigated the extraction of eight mono-, di- and trinitronaphthalenes from soil samples by ultrasonic, respectively, soxhlet extraction. Sonication was the more convenient procedure with a usually higher repeatability than the soxhlet method. All extracts were analysed by high-performance liquid chromatography with diode array detection. These methods were used to determine the concentration of nitronaphthalenes in five soil samples polluted by explosives. The most abundant contaminants were 1,5- and 1,8-dinitronaphthalene as well as 1,3,5-, 1,3,8- and 1,4,5-trinitronaphthalene. In all samples the sum of trinitronaphthalenes exceeded the sum of mono- and dinitronaphthalenes. It is recommendable to include these eight compounds in the analytical exploration of sites contaminated by explosives.

Chemistry Techniques, Analytical↗
PubMedDate not supplied

N-hydroxylation.

Explore the source record for details and available documents.

Amines↗
PubMed1985

The effect of diet on the mammalian gut flora and its metabolic activities.

The review will encompass the following points: A brief introduction to the role of the gut flora in the toxicology of ingested food components, contaminants, and additives, including known pathways of activation and detoxication of foreign compounds and the implication of the flora in enterohepatic circulation of xenobiotics. The advantages and disadvantages of the various methods of studying the gut flora (classical bacteriological techniques, metabolic and enzymological methods) will be critically discussed with special reference to their relevance to dietary, toxicological, and biochemical studies. Sources of nutrients available to the gut flora will be described including host products (mucus, sloughed mucosal cells, hormones, proteins) and exogenous nutrients derived from diet. An account of the problems involved in studies of dietary modification with special reference to the use of stock laboratory animal diets, purified diets, and human dietary studies. The influence of dietary modification on the flora will be assessed on the basis of changes in numbers and types of bacteria and their metabolic activity, drawing on data from human and animal studies. The effects of manipulation of the quantity and quality of protein, fat, and indigestible residues (fiber) of the diet will be described together with their possible implications for toxicity of ingested compounds.

Amino Acids↗
PubMed1998

Preparation of alkyl-substituted indoles in the benzene portion. Part 15. Asymmetric synthesis of (+)-duocarmycin SA using novel procedure for preparation of hydroxyindoles.

An asymmetric total synthesis of natural (+)-duocarmycin SA (1) starting from L-malic acid (7) was achieved as shown in Chart 5, establishing firmly the absolute configuration of 1. In order to find suitable reaction conditions for the key step, i.e., the formation of an alkoxyindole derivative, model compounds 9 and 40 were synthesized and two acetalization conditions using i) 2-ethyl-2-methyl-1,3-dioxane and boron trifluoride etherate, and ii) 1,3-bis(trimethylsilyloxy)propane and trimethylsilyl triflate were found to be effective. The former conditions were successfully applied to total synthesis and 49b was prepared from 48 in 54% yield. Further elaborations including i) Curtius rearrangement of 53b to 56, and ii) cleavage of the primary benzyloxy group in the presence of the secondary one in its close vicinity (56-->57) led to the relay compound 62, whose conversion to 1 has already been accomplished.

Alkylation↗