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Comparative Effects of Adriamycin and N-Trifluoroacetyladriamycin-14-valerate on Cell Kinetics, Chromosomal Damage, and Macromolecular Synthesis in Vitro¹

Comprehensive Cancer Center for the State of Florida, University of Miami Medical School, Miami, Florida 33101 [A. K., R. G.], and Sidney Farber Cancer Institute, Boston, Massachusetts 02115 [M. I., K. D.]

N-Trifluoroacetyladriamycin-14-valerate differs from Adriamycin in its rapid intracellular transport and lack of fluorescent binding to nuclei or chromosomes. Both of these anthracyclines cause inhibition in the incorporation of labeled precursors into nucleic acids, extensive chromosomal damage, and arrest of cell cycle traverse in G₂. In human lymphoid cells, N-trifluoroacetyladriamycin-14-valerate, unlike Adriamycin, does not show cell cycle phase-specific or proliferation-related cytotoxic effects. In an L1210 soft-agar assay, both Adriamycin and N-trifluoroacetyladriamycin-14-valerate show no enhanced sensitivity of mid-S-phase cells to their cytotoxic action.

¹ This investigation was supported by USPHS Grants CA19118, CA23688, and CA29360.

² To whom requests for reprints should be addressed, at Comprehensive Cancer Center for the State of Florida, University of Miami School of Medicine (R-71), P. O. Box 16960, Miami, Fla. 33101.

Received 10/12/78. Accepted 4/15/81.