title: Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives.
abstract: A series of pyrrolo[2,1,5-cd]indolizine derivatives has been synthesized and evaluated as ligands for the estrogen receptor. Properly substituted mono- and di-hydroxy derivatives showed binding in the low nanomolar range in accordance with their structural resemblance to estrogen.
authors.affiliation: Health Care Discovery and Preclinical Development, Novo Nordisk A/S, Målov, Denmark. asj@novo.dk
authors.forename: A S
authors.initials: AS
authors.lastname: Jørgensen
authors.forename: P
authors.initials: P
authors.lastname: Jacobsen
authors.forename: L B
authors.initials: LB
authors.lastname: Christiansen
authors.forename: P S
authors.initials: PS
authors.lastname: Bury
authors.forename: A
authors.initials: A
authors.lastname: Kanstrup
authors.forename: S M
authors.initials: SM
authors.lastname: Thorpe
authors.forename: L
authors.initials: L
authors.lastname: Naerum
authors.forename: K
authors.initials: K
authors.lastname: Wassermann
mesh_terms: D015195:Drug Design; D004958:Estradiol / Q000378:metabolism; D006801:Humans; D007212:Indolizines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D011960:Receptors, Estrogen / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D007212:Indolizines; D011758:Pyrroles; D011960:Receptors, Estrogen; D004958:Estradiol