Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives.
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.
Jørgensen
A S
AS
Health Care Discovery and Preclinical Development, Novo Nordisk A/S, Målov, Denmark. asj@novo.dk
Jacobsen
P
P
Christiansen
L B
LB
Bury
P S
PS
Kanstrup
A
A
Thorpe
S M
SM
Naerum
L
L
Wassermann
K
K
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
D007212:Indolizines; D011758:Pyrroles; D011960:Receptors, Estrogen; D004958:Estradiol