Potential DNA bis‐intercalating agents: Synthesis and antitumor activity of novel, conformationally restricted bis(9‐aminoacridines)

A series of bis(9‐aminoacridines) bridged by conformationally restricted tethers was synthesized and evaluated against L1210 in vitro. Several of these compounds were found to be highly active in this test system, with ID50 values below 10−7 M. CPK molecular models suggest that this antitumor activity can be correlated to the ability of these bis(9‐aminoacridines) to form bis‐intercalative complexes with DNA.