Hydantoins and their derivatives constitute a group of pharmaceutical compounds with anticonvulsant and antiarrhythmic properties, and are also used against diabetes. N-3 and C-5 substituted imidazolidines are examples of such products. As such, we have developed a synthesis of 2,4-dione and 2-thioxo-4-one imidazolidinic derivatives by reaction of amino acids with C-phenylglycine, phenyl isocya...

The preparation of a number of alkyl and alkoxy derivatives of pentacyclo[5.4.0.0.0.0]undecane8,11-dione derivatives utilising a cheap, practical, low energy, “green”, single-pass continuous flow photochemical reactor is reported Their H and C NMR spectra are fully assigned, revealing some general characteristics not previously reported for this class of compound, which should aid the assignmen...

Hydantoin derivatives, including phenytoin (5,5-diphenylhydantoin), have recently gained attention as they possess a variety of important biochemical and pharmacological properties. Nevertheless, available information on anticancer activity of hydantoin derivatives is still scarce. Here, we evaluated possible antileukemic potential of four phenytoin analogs, namely: methyl 2-(2,4-dioxo-5,5-diph...

A simple, novel, efficient and three-component procedure for the synthesis of pyrimido[4,5-d]pyrimidine-2,4-dione derivatives by the reaction of 6-amino-1,3-dimethyluracil, aldehyde and 2-benzylisothiourea hydrochloride promoted by ionic liquid 1-butyl-3-methylimidazolium bromide ([BMIm]Br) under solvent-free conditions is reported. The presented method is benefited from operational simplicity...

The receptor tyrosine kinase c-Met is an attractive target for therapeutic treatment of cancers nowadays. The discovery of small molecule inhibitors is of special interest in the blockade of the c-Met kinase pathway. Here, we initiated our study from compound 1a, a novel inhibitor against c-Met kinase. A substructure similarity search against the SPECS database and chemical synthesis methods we...

A simple and efficient strategy for the synthesis of indane-1,3-dione derivatives through a palladium(0)-catalyzed reaction incorporating tert-butyl isocyanide has been developed. In addition, by applying this protocol as the key step, indenopyrazole derivatives can be easily synthesized in high yields in a one-pot procedure. This methodology is tolerant of a wide range of substrates and applic...

A series of 2,3,4,9-tetrahydrofuro[2,3-b]quinolin-3,4-dione and ethyl 2-(substituted aniline) -4-oxo-4,5-dihydrofuran-3-carboxylate were synthesized and evaluated for cytotoxicity on murine leukemia WEHI-3 cells. The cytotoxic effects of most compounds tested were dose-dependent and the structure-activity relationships indicated that N-substituted benzyl derivatives displayed a stronger inhibit...

Five new diketopiperazine derivatives, (3Z,6E)-1-N-methyl-3-benzylidene-6-(2S-methyl-3-hydroxypropylidene)piperazine-2,5-dione (1), (3Z,6E)-1-N-methyl-3-benzylidene-6-(2R-methyl-3-hydroxypropylidene)piperazine-2,5-dione (2), (3Z,6Z)-3- (4-hydroxybenzylidene)-6-isobutylidenepiperazine-2,5-dione (3), (3Z,6Z)-3-((1H-imidazol-5-yl)-methylene)-6-isobutylidenepiperazine-2,5-dione (4), and (3Z,6S)-3-b...

In this paper we present the convenient syntheses of seven new phenyl hydrazin derivatives 8 (a-h). For this purpose, acenaphtho [1,2-e]-1,2,4-triazine-9(8H)-thione (3) was prepared, starting from acenaphthylene-1, 2-dione (1) and thiosemicabazide in good yield. The reaction of (3) with benzyl chloride resulted to synthesis of 9-(benzylthio)-acenaphtho[1,2-e]-1,2,4-triazines (5) that reacted wi...

A novel molecular scaffold, dihydropyridothienopyrimidin-4,9-dione, was synthesized from benzylamine or p-methoxybenzylamine in six steps involving successive ring closure to form a fused ring system composed of dihydropyridone, thiophene and pyrimidone. The pharmacological versatility of the dihydropyridothenopyrimidin-4,9-dione scaffold was demonstrated by inhibitory activity against metabotr...