Hycanthone analogs: dissociation of mutagenic effects from antischistosomal effects.
N-Oxidation at the diethylamino group of hycanthone, of lucanthone, and of two chlorobenzothiopyranoindazoles resulted in a marked reduction in mutagenic activity, while antischistosomal activity was retained or even enhanced. Introduction of chlorine into the 8-position of benzothiopyranoindazoles reduced acute toxicity but had no effect on chemnotherapeutic potency. These dissociations of biological activities indicate that safer antischistosomal compounds of this class can be developed.
D000818:Animals; D001681:Biological Assay; D005029:Ethylenediamines / Q000633:toxicity; D006801:Humans; D007928:Lethal Dose 50; D008154:Lucanthone / Q000494:pharmacology / Q000633:toxicity; D051379:Mice; D009153:Mutagens; D009154:Mutation / Q000187:drug effects; D051381:Rats; D012556:Schistosomicides / Q000633:toxicity; D013329:Structure-Activity Relationship; D013892:Thioxanthenes / Q000633:toxicity
D005029:Ethylenediamines; D009153:Mutagens; D012556:Schistosomicides; D013892:Thioxanthenes; D008154:Lucanthone