Analogues of hycanthone and lucanthone as antitumor agents.
Hycanthone analogues (5 and 6) containing 7-substituted hydroxyl groups were prepared and evaluated as antitumor agents. These compounds were significantly more active than the corresponding unsubstituted derivatives. The 7-hydroxylated 4-(hydroxymethyl)-9H-xanthen-9-ones, 11 and 12, were also active antitumor agents. However, the 7-hydroxy-9H-xanthen-9-one counterparts of the 7-hydroxylucanthones were totally devoid of antitumor activity. Results obtained thus far are consistent with the hypothesis that 4-hydroxymethyl substituents in the 9H-xanthen-9-one and 9H-thioxanthen-9-one series are required for antitumor activity.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006826:Hycanthone / Q000031:analogs & derivatives / Q000627:therapeutic use*; D007941:Leukemia P388 / Q000188:drug therapy; D008154:Lucanthone / Q000031:analogs & derivatives* / Q000627:therapeutic use; D051379:Mice; D013892:Thioxanthenes / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D013892:Thioxanthenes; D006826:Hycanthone; D008154:Lucanthone