Article ID Journal Published Year Pages File Type
1373063 Bioorganic & Medicinal Chemistry Letters 2008 7 Pages PDF
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
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