Hycanthone Analogs: Dissociation of Mutagenic Effects from Antischistosomal Effects

Science  15 Nov 1974:
Vol. 186, Issue 4164, pp. 647-648
DOI: 10.1126/science.186.4164.647


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.