Quantitative structure-activity relationship study on DNA-directed alkylating agents

A quantitative structure-activity relationship (QSAR) study is made on a series of antitumour aniline mustards and a series of acridine-linked aniline mustards. While cytotoxic activities of the former are found to depend only upon the electronic parameter, those of the latter are found to depend upon the lipophilicity of the linker chain and its connectivity index, thus suggesting that the linker chain probably facilitates the transport of the compounds to the DNA and helps them bind with the DNA.