EFFECTS OF N-TRIFLUOROACETYLADRIAMYCIN-14-VALERATE AND RELATED AGENTS ON DNA STRAND DAMAGE AND THYMIDINE INCORPORATION IN CCRF-CEM CELLS

  • 1 January 1979
    • journal article
    • research article
    • Vol. 39  (2) , 448-451
Abstract
N-Trifluoroacetyladriamycin-14-valerate (AD32) and N-trifluoroacetyladriamycin (AD41) were compared with adriamycin and daunorubicin in CCRF-CEM human lymphoblastic cells. All 4 agents produce DNA damage, as measured by alkaline unwinding methods. Thymidine incorporation, a measure of DNA synthesis, is inhibited by AD32 and AD41 and completely blocked by the other drugs. AD32 and AD41 inhibit growth of the cells after exposure for 2 h but are considerably less potent than is either adriamycin or daunorubicin. In drug uptake studies, cellular levels after 2 h incubations are lower for AD32 than for adriamycin, and both are severalfold lower than are those of daunorubicin. AD32 and AD41 (or their metabolites) may have DNA-related effects similar to those of adriamycin and daunorubicin. These common actions may be the proximal cytotoxic events for the 4 agents.