Antitumor Activity of Zindoxifene Derived Platinum Complexes View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

1988

AUTHORS

E. Von Angerer , N. Knebel , H. Schönenberger , J. Engel

ABSTRACT

Based on the new anti estrogen zindoxifene (1), cisdiaminodichloroplatinum(II) complexes were synthesized. Two of these complexes (1-Pt, 2-Pt) were studied in detail (Fig. 1). They showed high binding affinities for the estrogen receptor (RBA = 6.5 and 4.4 resp.; E2: RBA = 100) but were devoid of estrogenic or antiestrogenic activity in the mouse uterine weight test. Antineoplastic activity was evaluated in transplanted MXT mouse mammary tumors. The growth of hormone-independent tumors was not or only weakly inhibited, but both complexes showed a marked inhibition of hormone-sensitive tumors with T/C-values (mean tumor weight) between 11 and 23% following the administration of 3 × 20 mg/kg/ week for 6 weeks. The free ligands of the complexes were much less active. No cytostatic activity of the complexes was found in vitro with estrogen receptor negative human MDA-MB 231 breast cancer cells. However, the growth of hormone-dependent MCF-7 breast cancer cells was inhibited: Cell numbers were decreased by 52% and 66% resp. More... »

PAGES

761-762

Book

TITLE

Platinum and Other Metal Coordination Compounds in Cancer Chemotherapy

ISBN

978-1-4612-8967-8
978-1-4613-1717-3

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/978-1-4613-1717-3_90

DOI

http://dx.doi.org/10.1007/978-1-4613-1717-3_90

DIMENSIONS

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