In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for antiproliferative activities. All target compounds performed significantly inhibitory effects against wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) tumour cells (A431, A549, MCF-7, NCI-H1975). particular, compound 4d 3-flu...

The gas chromatographic properties of four derivatives of fatty acids (FA), namely fatty acid methyl esters, picolinyl esters, N-acyl pyrrolidides and 4,4-dimethyloxazoline derivatives, which contain various structural features (double bonds, branching, hydroxyl group) in their acyl chains have been compared on a low-polarity capillary column with a mass spectrometer as detector. Temperature pr...

3-Carboxy-1-sulfopyridin-1-ium chloride ([CPySO3H]+Cl-) as a novel ionic organocatalyst for thecondensation of aldehydes and 2-methylindole to synthesize bis(2-methyl-1H-indole) derivatives inacetonitrile at room temperature has been developed. Some tetrakis (2-methyl-1H-indole)derivatives have also been synthesized by the reaction of 2,2'-(butane-1,4-diylbis(oxy))dibenzaldehyde and 2-methylind...

A systematic study on the electrochemical behavior of the S-derivatives of 2-amino cyclopentene-1-dithiocarboxylic acid (ACDA) has been carried out in aqueous ethanolic solutions by means of polarography, coulometry and voltammetry. All the compounds studied exhibited a well defined anodic wave corresponding to a diffusion controlled process. Controlled potential coulometry gave n=1 per mol...

A simple and efficient method for the synthesis of 3-indolyl-3-hydroxy oxindoles and unsymmetrical 3,3-di(indolyl)indolin-2-ones using microwave irradiation without catalyst and solvent is described. A series of 3-indolyl-3-hydroxy oxindoles and unsymmetrical 3,3-di(indolyl)indolin-2ones have been synthesized in very short reaction times of 5 and 10 minutes and in yields ranging from 31% to 98%...

Methyl peroxy, a key radical in tropospheric chemistry, was recently shown to react with the hydroxyl radical at an unexpectedly high rate. Here, the molecular reaction mechanisms are elucidated using high-level quantum chemical methodologies and statistical rate theory. Formation of activated methylhydrotrioxide, followed by dissociation into methoxy and hydroperoxy radicals, is found to be th...

Many studies in vitro have implicated cytochrome oxidase and monoamine oxidase in the metabolism of epinephrine and other cateehol amines (2). However, no evidence for the participation of cytochrome oxidase in the metabolism of epinephrine in viva has been obtained. Furthermore, several investigations have indicated that monoamine oxidase plays only a minor role in the inactivation of epinephr...

Aedes albopictus (Skuse) is a widespread mosquito, vector of important human arboviruses, including Chikungunya, Dengue and Zika. It an extremely difficult species to control even for the onset resistances chemicals insecticides, therefore ecofriendly products are urgently needed. In this study, activity Amaryllidaceae alkaloids some their semisynthetic derivatives, 2-methoxy-1,4-naphthoquinone...

Tetrahydrobiopterin [(6R)-5,6,7,8-tetrahydro-L-biopterin, H(4)biopterin] is one of several cofactors of nitric oxide synthases (EC 1.14.13.39). Here we compared the action of N(5)-substituted derivatives on recombinant rat neuronal nitric oxide synthase with their effects on dihydropteridine reductase (EC 1.6.99.7) and phenylalanine hydroxylase (EC 1.14.16.1),the well-studied classical H(4)biop...

Background Vitex negundo L. has been widely studied for its beneficial effect in inflammatory and pain conditions. The present study describes the isolation of two new bioactive chromone constituents from V. negundo and their in vivo evaluation for anti-inflammatory and antinociceptive activities. Methods Two new chromone derivatives, namely, methyl 3-(2-(5-hydroxy-6-methoxy-4-oxo-4H-chromen-...