Acridine derivatives. IV. Synthesis, molecular structure, and antitumor activity of the novel 9‐anilino‐2,3‐methylenedioxyacridines

In the biological and physical investigation of a new class of deoxyribonucleic acid (DNA)‐intercalating antitumor agents, novel 9‐anilino‐2,3‐methylenedioxyacridines (twelve compounds) have been synthesized and evaluated for the activity against L1210 leukemia in vivo. A few of them possessed the same potency of the antitumor activity as 4′‐(9‐acridinylamino)methanesulfonyl‐m‐anisidine (amsacrine, m‐AMSA), which is an important antitumor agent in clinical use. The molecular structure of a typical one, 9a in this series have been determined by the X‐ray diffraction method using a single crystal. The results of this X‐ray investigation have shown that the new class of acridine derivatives have the methylenedioxy group fused at the 2‐ and 3‐positions of the acridine ring.