Preparation and evaluation of 2-substituted anthraquinones based on the anthracyclines

Abstract
Anthraquinones substituted at the 2 position with a basic side chain were prepared, and their binding to DNA was evaluated. All compounds showed an intercalative mode of binding to DNA; 1,4-dihydroxy derivatives bound more strongly than 1-hydroxy or nonhydroxylated compounds. Greatest DNA-binding activity was found where there were 5 atoms between the anthraquinone ring and the basic nitrogen. [The compounds prepared were tested for activity against P-388 leukemia in mice.].