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  • Title: Superiority of adriamycin-14-octanoate over adriamycin in reducing viability of methotrexate-resistant L5178Y cells: brief communication.
    Author: Hill BT, Price LA.
    Journal: J Natl Cancer Inst; 1977 Oct; 59(4):1311-4. PubMed ID: 561857.
    Abstract:
    Adriamycin-14-octanoate (ADR-OCT) was superior to adriamycin (ADR) in reducing the viability of L5178Y cells resistant to methotrexate (MTX). This effect was seen in logarithmically growing and plateau-phase cultures and increased both with dose and duration of exposure. Both ADR-OCT and ADR were effective inhibitors of the exogenous Escherichia coli DNA-dependent RNA polymerases in vitro and of the endogenous polymerase in mammalian cultured cells. Drug concentrations required for approximately 50% enzyme inhibition in both systems were comparable for both agents, being of the order of 10(-5) M. These experimental studies suggested that ADR-OCT may be a valuable agent for treating neoplasms resistant to MTX.
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