Dichloro[1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes: an approach to develop compounds with a specific effect on the hormone-dependent mammary carcinoma

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Abstract
Stereoisomeric dichloro[1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes [(.+-.)-dichloro[bis(4-hydroxyphenyl)ethylenediamine]platinum(II)] and their N,N''-dibutyl derivatives [dichloro[meso-N,N''-dibutyl-1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II)] were synthesized and tested on antitumor activity. The most active compound showed a modest inhibition of the [3H]estradiol receptor interaction and caused a marked effect on the growth of the hormone-dependent human MCF 7 breast cancer cell line. It was also active on the hormone-independent human MDA-MB 231 breast cancer cell line, on the ADJ/PC6 plasmacytoma of the Balb/C mouse, and on the L 5222 leukemia of the BD IX rat. Apparently the inhibition of the MCF 7 cell line is not mediated by the estrogen receptor system. Histopathological studies revealed very low toxicity.

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