Synthesis and antitumor activity of pyrido-amsacrine analogues and related compounds.

The pyrido derivatives of amsacrine [4'-(9-acridinylamino) methanesulfon-m-anisidine] were prepared and evaluated in the L1210 leukemia system. Almost all the pyrido analogues were tighter DNA-binding ligands than the corresponding amsacrine compounds. The significant inhibition of L1210 produced by pyrido-acridan-7-ones demonstrates that the anilino side chain is not essential for activity, although most of the compounds did not have improved activity compared with amsacrine.