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In Vitro Biological Evaluation of the R and S Isomers of 1-(Tetrahydrofuran-2-yl)-5-fluorouracil¹

Jerome P. Horwitz², J. Justin McCormick, Kerstin D. Philips, Veronica M. Maher, James R. Otto, David Kessel and Jií emlika

Research Division, Michigan Cancer Foundation [J. P. H., J. J. M., K. D. P., V. M. M., J. R. O., D. K., J. Z.], and the Departments of Oncology [J. P. H., D. K., J. .], and Pharmacology [D. K.], Wayne State University, School of Medicine, Detroit, Michigan 48201

The S isomer of Ftorafur was synthesized and the ability of the latter to inhibit growth of cultured human fibroblasts was determined relative to both the R isomer and the racemic mixture (Ftorafur) that is presently used clinically. No significant difference in the cytotoxic effects or the relative abilities to prevent an increase in cell numbers was observed with the three forms. Inhibition of DNA synthesis in murine L1210 leukemia cells by either isomer was observed only after prolonged (18-hr) exposure. The data suggest that Ftorafur is a repository form of 5-fluorouracil and that activity is manifested equally by both isomers.

¹ This investigation was supported in part by USPHS Research Grants CA 13858, CA 13058, and CA 16053 from the National Cancer Institute and in part by an institutional grant to the Research Division, Michigan Cancer Foundation, from the United Foundation of Greater Detroit. Presented in part at the 65th meeting of the American Association for Cancer Research (10).

² To whom requests should be addressed, at Research Division, Michigan Cancer Foundation, 110 E. Warren, Detroit, Mich. 48201.

Received 12/16/74. Accepted 2/ 7/75.