Schönenberger, Helmut and Wappes, B. and Jennerwein, M. and Berger, M. (1984) Development of selective, active platinum complexes. Contributions to oncology = Beiträge zur Onkologie 18 (Resistenzprobl. Chemo-Radiother. Malig. Tumoren), pp. 48-57.
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The development of Pt-complexes of the type 1,2-bis(4-hydroxyphenyl)ethylenediamines as ligands for estrogen receptors of receptor-pos. and -neg. mammary cancer cells is discussed. The degree of receptor affinity of the ligand was dependent on its configuration, i.e. the R,R- and the S,S-conformations, in contrast to the R,S conformation, were more effective for inhibition of estradiol-receptor interactions. An ethylenediamine structure was essential for antitumor activity of these compds. Exptl. results with various tumor systems demonstrated that R,R-dichloro-1,2-bis(4-hydroxyphenyl)ethylenediamine-Pt(II)-complex (I) [91326-63-5] was the most active compd. I as an antitumor drug seems promising since it has only slight nephrotoxic effects and no myelotoxic effects.
|Additional information (public):||CAN 102:89669 1-3 Pharmacology 7440-06-4D; 91265-66-6; 91326-62-4; 91326-63-5 Role: BIOL (Biological study) (neoplasm inhibitory activity of, estrogen receptor interaction and structure in relation to)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Receptors Role: BIOL (Biological study) (estrogen, platinum complexes interaction with, neoplasm-inhibiting activity in relation to) Neoplasm inhibitors (platinum complexes) Molecular structure-biological activity relationship (neoplasm-inhibiting, of platinum complexes) platinum complex antitumor structure estrogen receptor platinum complex antitumor|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||12 Nov 2010 09:57|
|Last Modified:||12 Nov 2010 09:57|
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