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 f rom optically active cyclic amino acids and amino alcohols is describe d. The absolute configurations of the target compounds were assigned b y X-ray and H-1-NMR analyses and by molecular modeling studies. The cy totoxic activity of the tricyclic derivatives was tested in vitro by g rowth inhibition assays using murine L1210 and human lymphoblastic CCR F-CEM leukemias. Compounds 5, 9, and 10 exhibited marked cytotoxic act ivity.