Over the years, the development of targeted medicines has made significant achievements. As a typical example, receptor tyrosine kinases (RTK) inhibitors have become important chemotherapy drugs for a variety of cancers. However, the effectiveness of these agents is always hindered by poor response rates and acquired drug resistance. In order to overcome these limitations, several dual-targeted...

Substituted 1, 2, 4Triazoles have shown multiple biological activities such as anti-inflammatory, anti fungal, etc. 5-mercapto triazoles were prepared from the potassium dithiocarbazinates. These triazoles were used for preparation of different derivatives by two different schemes. In the first scheme the Mannich bases were prepared from 5marcapto-s triazole Quinazolines. The 5-Marcato-s-Triazo...

Novel routes for the preparation of 2-amino-4H-pyran-3-carbonitrile 9, amino-arylbenzoic acid ester derivatives 13a,b, 2-aminotetrahydro-4H-chromene-3-carbonitrile 18, 3-amino-4-cyanotetrahydronaphthalene-2-carboxylic acid ester 26 and 4-amino-3,5-dicyanophthalic acid ester derivatives 37a-c were developed. The synthetic methods utilize one-pot reactions of acetylene carboxylic acid esters, α,β...

In an effort to develop anticancer agents, a series of Mannich bases were prepared by Mannich reaction. When one biologically active molecule is linked to another, the resultant molecule generally has increased potency. Hence two pharmacophores, i.e. quinazoline ring and amine moiety are fused to obtain highly potent, more specific and less toxic agent. In the present study, synthesis of novel ...

The behavior of 2-ethoxy-(4H)-3,1-benzoxazin-4-one (1) towards nitrogen nucleophiles, e.g. ethanolamine, aromatic amines (namely: p-toluidine, p-anisidine, p-hydroxyaniline, o-hydroxyaniline, o-bromoaniline, o-phenylenediamine, p-phenylenediamine, o-tolidinediamine) p-aminobenzoic acid, glucosamine hydrochloride, 2-aminonicotinic acid, 1-naphthalenesulfonic acid hydrazide, n-decanoic acid hydra...