Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375881 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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