Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.
A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay.
Smith
Roger A
RA
Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA.
Chen
Jinshan
J
Mader
Mary M
MM
Muegge
Ingo
I
Moehler
Ulrike
U
Katti
Suresh
S
Marrero
Diana
D
Stirtan
William G
WG
Weaver
Daniel R
DR
Xiao
Hong
H
Carley
William
W
D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D002460:Cell Line; D015195:Drug Design; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D006801:Humans; D008958:Models, Molecular; D020849:Raloxifene Hydrochloride / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000187:drug effects; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*
D001572:Benzofurans; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D020849:Raloxifene Hydrochloride