title: SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists.
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.
authors.affiliation: Department of Medicinal Chemistry, N.V. Organon, PO Box 20, 5340 BH Oss, The Netherlands.
authors.forename: Paul P M A
authors.initials: PP
authors.lastname: Dols
authors.forename: Brigitte J B
authors.initials: BJ
authors.lastname: Folmer
authors.forename: Hans
authors.initials: H
authors.lastname: Hamersma
authors.forename: Cor W
authors.initials: CW
authors.lastname: Kuil
authors.forename: Hans
authors.initials: H
authors.lastname: Lucas
authors.forename: Lourdes
authors.initials: L
authors.lastname: Ollero
authors.forename: Jos B M
authors.initials: JB
authors.lastname: Rewinkel
authors.forename: Pedro H H
authors.initials: PH
authors.lastname: Hermkens
mesh_terms: D000081:Acetamides; D001665:Binding Sites; D005463:Fluoroacetates; D008958:Models, Molecular; D010077:Oxazepines / Q000737:chemistry* / Q000494:pharmacology*; D011374:Progesterone / Q000737:chemistry; D011980:Receptors, Progesterone / Q000819:agonists*; D013329:Structure-Activity Relationship; D014269:Trifluoroacetic Acid / Q000737:chemistry
chemical_list: D000081:Acetamides; D005463:Fluoroacetates; D010077:Oxazepines; D011980:Receptors, Progesterone; C030688:trifluoroacetamide; D011374:Progesterone; D014269:Trifluoroacetic Acid