High-performance liquid chromatography in stability studies of an organophosphorus insecticide in free form and after formulation as emulsifiable conce

DCPE [α-(diethoxyphosphinoximino)dicyclopropylmethane] is an organophosphorus compound with good insecticidal activity. It is a yellow oily liquid, p. © 1994

Synthesis and antifungal activity of some alkynylthio compounds

Some 4-(p-alkoxyphenylthio)but-2-yn-yl-amine hydrochlorides and 4-(p-alkoxyphenylthio)prop-1-yn-yl-iodides were prepared and tested for their antifungal activity. All the tested compounds were active in inhibiting the growth of 4 fungal types. The iodine compounds were the more effective. © 1992

Use of reversed-phase high-performance liquid chromatography in lipophilicity studies of 9H-xanthene and 9H-thioxanthene derivatives containing an aminoalkanamide or a nitrosoureido group. Comparison between capacity factors and calculated octanol-water partition coefficients

The lipophilicity of 9H-xanthene and 9H-thioxanthene derivatives, containing either a basic alkanamide or a nitrosoureido group, was studied by means of reversed-phase high-performance liquid chromatography using an octadecylsilane stationary phase, methanol as organic modifier and n-decylamine as a masking agent. Correlation of the extrapolated capacity factors with log P values calculated according to Rekker's fragmental system showed an excellent parallelism between HPLC and the octanol-water partition system and permitted the generation of a hydrophobic fragmental constant for the nitrosoureido group. Tetrahydrofuran was also tried as an organic modifier but without satisfactory results. © 1993

Synthesis and Antitumor Activity of Some New 2‐Chloroethylnitrosoureas

The synthesis of a series of N‐(2‐chloroethyl)‐N′‐(9H‐xanthen‐9‐yl)‐N‐nitrosoureas and N‐(2‐chloroethyl)‐N′‐(9H‐thioxanthen‐9‐yl)‐N‐nitrosoureas is described. The title compounds were evaluated against NSCLCN6 L16 bronchial epidermoid carcinoma in vitro and some of them were found to be active. N‐(2‐chloroethyl)‐N′‐(2‐methoxy‐9H‐xanthen‐9‐yl)‐N‐nitrosourea (8e) was active against leukemia P388 tumor system in mice. Copyright © 1993 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinhei

Synthesis and antiviral activity of some new 1H-1,2,4-triazole derivatives

A series of new 1H-1,2,4-triazole derivatives was synthesised and evaluated in vitro for activity against various DNA and RNA viruses. Compounds 1-benzyl-5-(4-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 2b, 1-benzyl-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 2c and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 4h proved active against reovirus-1, and compounds 1-[(2-hydroxyethoxy)methyl]-5-phenyl-3-(2-pyrazinyl)-1H-1,2,4-triazole 4f and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 4h against parainfluenza-3 virus, in Vero cells at concentrations that were 5- to 40-fold lower than the cytotoxic concentration required to alter normal cell morphology. © 1994

New aza-thioxanthones: Synthesis and cytotoxicity

A new series of aza-thioxanthones has been synthesized and tested for in vitro cytotoxicity in a number of cell lines. Almost all the compounds were found to exhibit significant cytotoxicity in the leukemic MOLT-4 line, whereas some of them showed pronounced activity in the non-small lung cancer cell line HOP-92

Synthesis of N‐(9H‐Xanthen‐9‐yl)aminoalkanamide and N‐(9H‐Thioxanthen‐9‐yl)aminoalkanamide Derivatives and their in vitro Evaluation as Potential Intercalators and Antitumor Drugs

A series of new N‐(9H‐xanthen‐9‐yl)aminoalkanamide and N‐(9H‐thio‐xanthen‐9‐yl)aminoalkanamide derivatives was synthesized and evaluated as potential intercalators by measuring their DNA binding affinity. They were also tested for cytotoxic activity against L1210. The results suggest that the cytotoxicity of these molecules was not due to an intercalating mechanism. Copyright © 1994 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinhei