Spruss, Thilo and Schertl, Sabine and Schneider, Martin R. and Gust, Ronald and Bauer, Kurt and Schönenberger, Helmut (1993) [Meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] -dichloroplatinum(II), a new drug not only parenterally but also orally active in the therapy of breast and prostate cancer. Journal of cancer research and clinical oncology 119 (12), pp. 707-716.
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The platinum complex [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)- ethylenediamine]dichloroplatnum(II), K, was tested for its antitumor activity on hormone-sensitive tumor models under peroral administration. The resorption from the gastrointestinal tract was proved by detg. the estrogenic effect of K in a dose/activity study using the immature-mouse uterine wt. test. In comparison to the s.c. 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 s.c. 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 NbR prostatic carcinoma of the rat. Histol. examns. showed that the platinum complex K did not cause cisplatin-like kidney damage or irritations of gastric or intestinal mucosa when given perorally.
|Additional information (public):||CAN 120:260726 1-6 Pharmacology 105856-23-3; 111086-58-9 Role: BIOL (Biological study) (breast and prostate cancer inhibition by); 15663-27-1 (Cisplatin) Role: BIOL (Biological study) (breast and prostate cancer inhibition by mesodichlorohydroxyphenylethylenediaminedichloroplatinum(II) vs.)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Neoplasm inhibitors (mammary gland, orally active mesodichlorohydroxyphenylethylenediaminedichloroplatinum(II) Mammary gland Prostate gland (neoplasm, inhibitors, orally active mesodichlorohydroxyphenylethylenediaminedichloroplatinum(II) Neoplasm inhibitors (prostate gland, orally active mesodichlorohydroxyphenylethylenediaminedichloroplatinum(II) platinum complex antitumor breast prostate cancer|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||10 Nov 2010 13:06|
|Last Modified:||12 Nov 2010 07:21|
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