An efficient one-pot three-component protocol for the synthesis of novel tetrahydrobenzofuran-chromone conjugates using 3-formylchromones and 1,3-cyclohexandiones in presence a variety alkyl or aryl isocyanides was developed. The reaction sequence consists an initial Knoevenagel condensation aromatic aldehydes with 1,3-cyclohexandione derivatives, followed by [4 + 1] cycloaddition isocyanides, ...

Several new 3-formylchromone derivatives proved to be modifiers of multidrug resistance in mouse lymphoma cells and in human Colo320 colon cancer cells. There is apparently a structure-activity relationship between the antiproliferative multidrug resistance-reversing effect and the chemical structure of the 3-formylchromones. The total polar surface areas and the ground state dipole moments of ...

Several 3-formylchromone derivatives were examined for their tumor cell-cytotoxic, anti-Helicobacter pylori, urease inhibitory and anti-HIV activity. Comparing their relative cytotoxicity against four human tumor cell lines and three normal human cells, tumor cell-specific cytotoxicity was detected in some 3-formylchromone derivatives. There was no clear-cut relationship between the cytotoxicit...

Novel substituted 1,2,4-dithiazolylchromones 3a-j were synthesized by the reaction of 3-formylchromones (1a-j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, (1)H and (13)C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains...

We report the antimicrobial activity of formylchromones. These compounds are remote structural analogues of nalidixic acid and quinolone antibiotics, and their activity was investigated by a simple micro-scale method designed for the determination of minimal inhibitory concentrations (MIC) of drug candidates and antibiotics against aerobic bacteria and yeasts. Minimal bactericidal and fungicida...