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

URN to cite this document:: urn:nbn:de:bvb:355-epub-157755
DOI to cite this document:: 10.5283/epub.15775

Angerer, S. von ; Brandl, G. ; Mannschreck, Albrecht ; Weimar, C. ; Wiegrebe, Wolfgang

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Date of publication of this fulltext: 12 Jul 2010 07:38

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Item type:	Article
Journal or Publication Title:	Anti-Cancer Drug Design
Volume:	7
Page Range:	pp. 351-363
Date:	1992
Institutions:	Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Wiegrebe
Keywords:	cytostatic activity/dibenzo[a,g]quinolizin-8-ones/estrogen receptor affinity/synthesis
Dewey Decimal Classification:	500 Science > 540 Chemistry & allied sciences
Status:	Published
Refereed:	Yes, this version has been refereed
Created at the University of Regensburg:	Unknown
Item ID:	15775

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Abstract

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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