The synthesis of radiosensitizers designed to bind to the minor groove of duplex DNA

Abstract

The synthesis is described of novel compounds, 17, 21, 25 and 27, containing in their molecular architecture both a terminal nitroarene component and an oligopeptide similar to that in the antibiotic distamycin, which is known to bind into the minor groove of duplex DNA. It is hoped that the compounds may concentrate around DNA in cells and so potentiate the action of the nitroarene as a radiosensitizer.