Cytotoxicities of 93 quinazoline derivatives against HeLa cells have been determined as the isoeffective concentrations inhibiting, after a single dose, the protein synthesis to 50% of the control amount after 48 h incubation. The dependence of cytotoxicity on hydrophobicity of the studied derivatives has been described using a previously published model-based approach. The studied derivatives are classified into nine classes each forming a smooth hydrophobicity-cytotoxicity curve. Owing to the acceptable agreement between the model and the data it can be inferred that: (1) the compounds except two derivatives bind to the receptors with approximately the same affinity; (2) the criterion for the classification is the different rate of metabolism. The results represent a basis for a rational development of more potent quinazoline derivatives.

Department of Biochemistry and Microbiology Faculty of Chemical Technology Slovak Technical University Bratislava Slovakia

Antibacterial effects of trisubstituted quinazoline derivatives

Antibacterial effect of some substituted tricyclic quinazolines and their synthetic precursors

Antibacterial effect of some 2,6-disubstituted 4-anilinoquinazolines