SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists
| Autor: | Hans Hamersma, Johannes Bernardus Maria Rewinkel, Paul Peter Marie Antonius Dols, Hans Lucas, Cor W. Kuil, Pedro H. H. Hermkens, Lourdes Ollero, Folmer Brigitte Johanna Bernita |
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| Rok vydání: | 2008 |
| Předmět: |
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Molecular Agonist medicine.drug_class Stereochemistry Fluoroacetates Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis D-1 Structure-Activity Relationship Acetamides Drug Discovery Progesterone receptor medicine Trifluoroacetic Acid Structure–activity relationship Binding site Receptor Molecular Biology Progesterone Binding Sites Chemistry Organic Chemistry In vitro Oxazepines Molecular Medicine Receptors Progesterone |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:1461-1467 |
| ISSN: | 0960-894X |
| Popis: | 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: | OpenAIRE |
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