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.

Graphical abstractWe report the synthesis of N-substituted-2-phenylindoles as estrogen receptor ligands. Optimal tether lengths were explored for creating a PAMAM-conjugated indole ligand.Figure optionsDownload full-size imageDownload as PowerPoint slide