Angerer, Erwin von (1982) Effect of N,N'-diethyl-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines on the 7,12-dimethylbenz[a]anthracene-induced mammary carcinoma of the rat. Journal of medicinal chemistry 25 (11), pp. 1374-1377.
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The syntheses and estrogen receptor affinities of meso- and (+/-)-N,N'-dialkyl-1,2-bis(2,6-dichloro-4-hydroxypheny)ethylenediamines (2) are described. They show high binding affinities in both diastereomeric forms but with a preference for the meso isomer, reaching a RBA value of 8.6 (meso-2b; 17 beta-estradiol = 100). Both stereoisomers of 2b exhibit a strong inhibitory effect on the 7,12-dimethylbenz[alpha]anthracene (DMBA) induced hormone-dependent mammary carcinoma of the Sprague-Dawley rat, reducing the tumor area by 74 (meso-2b) and 24% [(+/-)-2b], respectively, after 4 weeks administration of 6 x 6 (mg/kg)/week. The high uterotrophic potency makes a mode of action likely which corresponds to the effect of high doses of estrogens.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||03 Dec 2008 15:49|
|Last Modified:||05 Aug 2009 13:48|