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Bioorg Med Chem Lett. 2003 Jun 2;13(11):1907-10.

Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).

Author information

1
Discovery Chemistry Research and Technologies, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. wallace_owen@lilly.com

Abstract

A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay.

PMID:
12749895
DOI:
10.1016/s0960-894x(03)00306-8
[Indexed for MEDLINE]

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