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Science 15 November 1974:
Vol. 186. no. 4164, pp. 647 - 648
DOI: 10.1126/science.186.4164.647
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Articles

Hycanthone Analogs: Dissociation of Mutagenic Effects from Antischistosomal Effects

Peter B. Hulbert 1, Philip E. Hartman 1, and Ernest Bueding 1

1 John Hopkins University Baltimore, Maryland 21205

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.

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Science. ISSN 0036-8075 (print), 1095-9203 (online)