Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373063 | Bioorganic & Medicinal Chemistry Letters | 2008 | 7 Pages |
Abstract
We have developed a new class of progesterone receptor agonists having a tetracyclic dibenzo-oxazepine structure 1. In this paper, the synthesis and structure–activity relationships of this new class are described. This work led to the identification of potent progesterone agonists up to 1 nM activity. Substitution at positions 6, 7 and 1 has proven to be crucial for activity, indicating that probably these positions are involved in important interactions with the receptor.
Graphical abstractThe synthesis and SAR of a new class of non-steroidal progesterone receptor agonists having a tetracyclic dibenzo-oxazepine structure are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Paul P.M.A. Dols, Brigitte J.B. Folmer, Hans Hamersma, Cor W. Kuil, Hans Lucas, Lourdes Ollero, Jos B.M. Rewinkel, Pedro H.H. Hermkens,