Angerer, Erwin von (1982) Effect of N,N'-diethyl-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines on the DMBA-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-hydroxypheny1)
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@-estradiol=1 00). Both stereoisomers
of 2b exhibit a strong inhibitory effect on the 7,12-dimethylbenz[a]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 > 540 Chemistry & allied sciences|
|Created at the University of Regensburg:||Unknown|
|Deposited On:||17 May 2010 12:14|
|Last Modified:||20 Jul 2011 22:28|