Title of article
SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists
Author/Authors
Paul P.M.A. Dols، نويسنده , , Brigitte J.B. Folmer، نويسنده , , Hans Hamersma، نويسنده , , Cor W. Kuil، نويسنده , , Hans Lucas، نويسنده , , Lourdes Ollero، نويسنده , , Jos B.M. Rewinkel، نويسنده , , Pedro H.H. Hermkens، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
7
From page
1461
To page
1467
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.
Keywords
progesterone receptor , agonist , Non-steroidal
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799187
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