Tethered indoles as functionalizable ligands for the estrogen receptor.
To create ligands for the estrogen receptor that contain pendant groups for tethering to a poly(amido)amine (PAMAM) dendrimer, we have explored a class of N-substituted 2-phenyl indoles. Attachment of tethers of different length and chemical nature to this non-steroidal indole scaffold gave high affinity ligand-tether conjugates that can be easily functionalized. To further explore the utility of this system, an indole-conjugated dendrimer was prepared and evaluated as an estrogen receptor ligand.
Trogden
Bridget G
BG
Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.
Kim
Sung Hoon
SH
Lee
Shuyi
S
Katzenellenbogen
John A
JA
D050091:Dendrimers; D007211:Indoles / Q000378:metabolism*; D008024:Ligands; D011073:Polyamines / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism*
D050091:Dendrimers; D007211:Indoles; D008024:Ligands; C104700:PAMAM Starburst; D011073:Polyamines; D011960:Receptors, Estrogen