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  • 1
    ISSN: 1432-1335
    Keywords: Platinum complex ; Peroral administration ; Estrogenic activity ; Antitumor activity ; MXT(M3.2) mouse mammary tumor ; Noble Nb-R rat prostatic tumor ; Toxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The platinum complex [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)-ethylenediamine]dichloroplatinum(II), K, was tested for its antitumor activity on hormonesensitive tumor models under peroral administration. The resorption from the gastrointestinal tract was proved by determining the estrogenic effect of K in a dose/activity study using the immature-mouse uterine weight test. In comparison to the subcutaneous injection, a tenfold peroral dose was administered to achieve identical effects. By peroral treatment of the hormone-sensitive MXT(M3.2) mammary carcinoma of the mouse with K an almost complete inhibition of the tumor growth was obtained. This effect was superior to that of subcutaneously applied cisplatin and significantly better than that obtained by perorally administered ligand L at an equimolar dose, indicating that the antitumor effect is caused by the intact complex K and not by the liberated ligand L. The strong antitumor activity of perorally applied K was also demonstrated on the hormone-sensitive Noble Nb-R prostatic carcinoma of the rat. Histological examinations showed that the platinum complex K did not cause cisplatin-like kidney damage or irritations of gastric or intestinal mucosa when given perorally.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1335
    Keywords: 2-Phenylindole ; Antitumor activity ; Estrogen-dependent mammary tumors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The antineoplastic activity of 4-chloro-2-(2,6-dichloro-4-hydroxyphenyl)-1-ethyl-6-hydroxyindole (D 15413) was determined in several estrogen-dependent mammary tumor models. The growth of DMBA-induced rat mammary carcinomas was inhibited by doses ranging from 2 to 18 mg/kg. A dose of 6×12 mg/kg per week p.o. reduced the tumor area by 82% (control+192%). D 15413 was also active against MNU-induced rat mammary tumors and transplanted MXT tumors of the mouse. In vitro, the growth of estrogen receptor positive MCF-7 breast cancer cells was inhibited by D 15413 (10−8–10−5 M). A mode of action considering endocrine and cytotoxic effects is discussed.
    Type of Medium: Electronic Resource
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