Nitro and amino derivatives of lucanthone as antitumor agents.
A group of nitro and amino derivatives of lucanthone was prepared and tested for antitumor activity. Reaction of 1-chloro-4-methyl-7-nitrothioxanthenone and N,N-diethylethylenediamine gave the 7-amino analogue (11) directly, accompanied by 7-amino-1-chloro-4-methylthioxanthenone. The antitumor activity of 11 was inferior to that of lucanthone and 7-hydroxylucanthone. The most active compound in the series was the nitro compound 1. In the P-388 lymphocytic leukemia screen it showed a T/C = 178 at 200 mg/kg.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D007941:Leukemia P388 / Q000188:drug therapy; D008154:Lucanthone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice
D000970:Antineoplastic Agents; D008154:Lucanthone