SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists
Paul P M A Dols1, Brigitte J B Folmer, Hans Hamersma
1Department of Medicinal Chemistry, N.V. Organon, PO Box 20, 5340 BH Oss, The Netherlands.
Bioorganic & Medicinal Chemistry Letters
|January 30, 2008
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.
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