Tethered indoles as functionalizable ligands for the estrogen receptor

Bridget G. Trogden; Sung Hoon Kim; Shuyi Lee; John A. Katzenellenbogen

doi:10.1016/j.bmcl.2008.11.043

Tethered indoles as functionalizable ligands for the estrogen receptor

Bridget G. Trogden, Sung Hoon Kim, Shuyi Lee, John A. Katzenellenbogen

Chemistry

Research output: Contribution to journal › Article › peer-review

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.

Original language	English (US)
Pages (from-to)	485-488
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2008.11.043
State	Published - Jan 15 2009

Keywords

Estrogen receptor
Indole
PAMAM dendrimer

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Online availability

10.1016/j.bmcl.2008.11.043

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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.",

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note = "Funding Information: This research was supported by a Grant from the NIH (PHS 5R37 DK15556). We thank Drs. F. Stossi and B. Katzenellenbogen for performing co-transfection assays and Kathryn Carlson for the binding assays. ",

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AU - Trogden, Bridget G.

AU - Kim, Sung Hoon

AU - Lee, Shuyi

AU - Katzenellenbogen, John A.

N1 - Funding Information: This research was supported by a Grant from the NIH (PHS 5R37 DK15556). We thank Drs. F. Stossi and B. Katzenellenbogen for performing co-transfection assays and Kathryn Carlson for the binding assays.

PY - 2009/1/15

Y1 - 2009/1/15

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Tethered indoles as functionalizable ligands for the estrogen receptor

Abstract

Keywords

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