EFFECT OF 4'-DOXORUBICIN ANALOGS ON HETERO-TRANSPLANTATION OF HUMAN-TUMORS IN CONGENITALLY ATHYMIC MICE

  • 1 January 1981
    • journal article
    • research article
    • Vol. 65  (11-1) , 1063-1075
Abstract
The antitumor activity of 3 new doxorubicin (DX) derivatives with less cardiotoxicity than the parent compound was tested against several human tumors representative of some of the major classes of human cancer. The tested DX derivatives, modified on the 4'' position of the amino sugar, were 4''-epiDX, 4''-deoxyDX and 4''-O-methylDX. Fourteen human tumors (3 breast tumors, 3 lung tumors, 3 melanomas, 2 ovarian tumors, 1 prostate tumor, 1 sarcoma and 1 larynx tumor) serially transplanted in athymic mice were used to screen the antineoplastic activity of the 4''-DX derivatives. BALB/c nude mice were treated i.v. with equitoxic doses of each as a single agent (.ltoreq. LD10 [10% LD]) on a weekly basis for 3-4 wk, starting when the tumor became relatively large. 4''-EpiDX, which has a higher threshold limit of cardiac toxicity in man, was active against breast, lung (epidermoid and oat cell carcinoma), prostate and ovarian tumors. This drug showed particularly good activity against melanomas. 4''-DeoxyDX was active against breast and prostate tumors; 4''-O-methylDX was active against breast and ovarian tumors and possibly sarcoma.

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