Fluorescent anticancer quinazolines as molecular probes for ß-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites

Abstract : Anticancer 2-aminoquinazolines were evaluated by their photophysical properties responding to media changes. By binding to the colchicine binding site of β-tubulin, the fluorescence emission of 2-N-morpholino-derivative (1) was blue-shifted with enhanced intensity. These distinguished features were used for the development of a β-tubulin colchicine site competition assay and visualization of the intracellular distribution of 1 by fluorescence microscopy.