ACRIDINE-DERIVATIVES .4. 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.