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Mutagenicity of Heterocyclic Nitrogen Mustards (ICR Compounds) in Cultured Mammalian Cells¹

University of Tennessee-Oak Ridge Graduate School of Biomedical Sciences, and Biology Division, Oak Ridge National Laboratory,⁴ Oak Ridge, Tennessee 37830

The mutagenicity of six heterocyclic nitrogen mustards (ICR compounds) has been determined in a cultured mammalian cell system by use of resistance to the purine analog 6-thioguanine to select for mutation induction at the hypoxanthine-guanine phosphoribosyltransferase locus in Chinese hamster ovary cells. The six compounds tested are ICR 191, 170, 292, 372, 191-OH, and 170-OH. The first four contain a single 2-chloroethyl group (nitrogen half-mustard) on the side chain and are mutagenic, with the tertiary amine types (170 and 292) 3 to 5 times more mutagenic than the secondary amine types (191 and 372). The remaining two compounds (191-OH and 170-OH) are not mutagenic, indicating that the 2-chloroethyl group is needed for mutation induction.

¹ By acceptance of this article, the publisher or recipient acknowledges the right of the U. S. Government to retain a nonexclusive, royalty-free license in and to any copyright covering the article.

² Recipient of Carcinogenesis Training Grant CA 05296 from the National Cancer Institute.

³ Predoctoral fellow; recipient of Grant CA 09104 from the National Cancer Institute.

⁴ Operated by Union Carbide Corporation for the Department of Energy.

Received 7/28/77. Accepted 11/22/77.

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