THIOANALOGS OF ANTITUMOR ANTIBIOTICS .2. SYNTHESIS AND PRELIMINARY INVITRO CYTOTOXICITY EVALUATION OF TRICYCLIC [1,4]BENZOTHIAZEPINE DERIVATIVES

The synthesis of tricyclic [1,4]benzothiazepine derivatives starting from optically active cyclic amino acids and amino alcohols is described. The absolute configurations of the target compounds were assigned by X-ray and H-1-NMR analyses and by molecular modeling studies. The cytotoxic activity of the tricyclic derivatives was tested in vitro by growth inhibition assays using murine L1210 and human lymphoblastic CCRF-CEM leukemias. Compounds 5, 9, and 10 exhibited marked cytotoxic activity.