Tethered indoles as functionalizable ligands for the estrogen receptor

…, SH Kim, S Lee, JA Katzenellenbogen

Index: Trogden, Bridget G.; Kim, Sung Hoon; Lee, Shuyi; Katzenellenbogen, John A. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 485 - 488

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Citation Number: 9

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 ...