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  • Title: Improved antitumor effects of 3'-deamino-3'-morpholino derivatives of pirarubicin.
    Author: Ajito K, Ikeda D, Nosaka C, Komuro K, Kondo S, Takeuchi T.
    Journal: J Antibiot (Tokyo); 1990 Nov; 43(11):1464-70. PubMed ID: 2272921.
    Abstract:
    The preparation and antitumor effects of 3'-deamino-3'-morpholino derivatives of pirarubicin are described. Di-N-alkylation of pirarubicin with bis(2-iodoethyl)ether gave 3'-morpholino-pirarubicin, which was converted into its 13-tosylhydrazone, 13-deoxy derivative and 13-(S)- and 13-(R)-dihydro derivatives. Intraperitoneal administration to murine tumors indicated that the effective dose ranges of the compounds having sp3 carbon at C-13 position were broader than those of the compounds having sp2 carbon. By oral administration, 13-(S)-dihydro isomer was more effective than 13-(R)-dihydro isomer.
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