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Investigation of the Configurational and Conformational Influences on the Hormonal Activity of 1,2-Bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and of their Platinum(II) Complexes. 1. Synthesis, Estradiol Receptor Affinity, and Estrogenic Activity of Diastereomeric [N-Alkyl- and N,N'-Dialkyl-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) Complexes

Gust, Ronald ; Niebler, Karlheinz ; Schönenberger, Helmut



Abstract

N-Monoalkylated (Et) and N,N'-dialkylated (Me and Et) 1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and their dichloroplatinum(II) complexes were synthesized, and their configuration and conformational behavior were 1H-NMR spectroscopically clarified. The latter was brought in relation to their relative binding affinity (RBA) to the estrogen receptor as well as to their estrogenic ...

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