title: Tethered indoles as functionalizable ligands for the estrogen receptor.
abstract: 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.
authors.affiliation: Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.
authors.forename: Bridget G
authors.initials: BG
authors.lastname: Trogden
authors.forename: Sung Hoon
authors.initials: SH
authors.lastname: Kim
authors.forename: Shuyi
authors.initials: S
authors.lastname: Lee
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
mesh_terms: D050091:Dendrimers; D007211:Indoles / Q000378:metabolism*; D008024:Ligands; D011073:Polyamines / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism*
chemical_list: D050091:Dendrimers; D007211:Indoles; D008024:Ligands; C104700:PAMAM Starburst; D011073:Polyamines; D011960:Receptors, Estrogen