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Carcinogenicity of Derivatives of 7,12-Dimethylbenz(a)anthracene¹

Departments of Pharmacology and Medicine, University of Kentucky College of Medicine, Lexington, Kentucky 40506

Eleven derivatives of 7,12-dimethylbenz(a)anthracene were tested for carcinogenicity in Sprague-Dawley female rats by the s.c. injection of 1.0 or 0.1 mg of compound dissolved in 0.1 ml of sesame oil on alternate days for 20 doses. Eight derivatives [7-hydroxymethyl-12-methyl-, 7-formyl-12-methyl-, 7-methoxymethyl-12-methyl-, 7-acetoxymethyl-12-methyl-, 7-benzoyloxymethyl-12-methyl-, 7-iodomethyl-12-methyl-, 7-bromomethyl-12-methyl,- and 7-chloromethyl-12-methylbenz(a)anthracene] were carcinogenic at the 1-mg dose level, and 5 [benzoyloxymethyl-12-methyl-, 7-formyl-12-methyl-, 7-bromomethyl-12-methyl-, 7-hydroxymethyl-12-methyl-, and 7-iodomethyl-12-methylbenz(a)anthracene] were carcinogenic at the 0.1-mg dose level (200 days of observation). These observations suggest that the formation of 7-hydroxymethyl-12-methylbenz(a)anthracene may be the first step in the chain of events which result in cancer caused by these polycyclic hydrocarbons.

¹ Supported by Grant E307 from the American Cancer Society and presented in part at the Tenth International Cancer Congress, Abstracts, No. 92, p. 60, Houston, Texas, 1970.

Received 5/ 5/71. Accepted 7/21/71.

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