| Autor: |
Dols PP; Department of Medicinal Chemistry, N.V. Organon, PO Box 20, 5340 BH Oss, The Netherlands., Folmer BJ, Hamersma H, Kuil CW, Lucas H, Ollero L, Rewinkel JB, Hermkens PH |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 15; Vol. 18 (4), pp. 1461-7. Date of Electronic Publication: 2007 Dec 28. |
| DOI: |
10.1016/j.bmcl.2007.12.065 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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