Comparative effects of adriamycin and N-trifluoroacetyladriamycin-14-valerate on cell kinetics, chromosomal damage, and macromolecular synthesis in vitro.

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.