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Dibenzo[a,g]quinolizin-8-ones: synthesis, estrogen receptor affinities, and cytostatic activity

URN to cite this document:
Angerer, S. von ; Brandl, G. ; Mannschreck, Albrecht ; Weimar, C. ; Wiegrebe, Wolfgang
Date of publication of this fulltext: 12 Jul 2010 07:38


A number of acetoxy-substituted dibenzo[a,g]quinolizin-8-ones were synthesized by the reaction of 1-oxoisoquinolines with substituted homophthalic acid anhydride. All of the derivatives with acetoxy groups in positions 3 and 10 bind to the estrogen receptor. Relative binding affinities (RBA) ranged from 1.8 to 5.6 (estradiol: RBA = 100) when the substituent at C-6 was a short alkyl group. ...


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