Abstract
The estrogen receptor (ER), a member of the nuclear receptor (NR) family, is involved in the regulation of physiological effects such as reproduction and bone homeostasis. Approximately 70% of human breast cancers are hormone-dependent and ERα-positive, and, thus, ER antagonists are broadly used in breast cancer therapy. We herein designed and synthesized a set of ER antagonists with a 4-heterocycle-4-phenylheptane skeleton.
Keywords:
Antagonist; Estrogen receptor; Heterocycles.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Drug Design
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Estrogen Receptor Antagonists / chemical synthesis
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Estrogen Receptor Antagonists / chemistry
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Estrogen Receptor Antagonists / pharmacology*
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Heptanes / chemical synthesis
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Heptanes / chemistry
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Heptanes / pharmacology*
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Ligands
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MCF-7 Cells
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Models, Molecular
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Molecular Structure
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Receptors, Estrogen / antagonists & inhibitors*
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Receptors, Estrogen / metabolism
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / chemistry
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Thiophenes / pharmacology*
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Tumor Cells, Cultured
Substances
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Estrogen Receptor Antagonists
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Heptanes
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Indoles
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Ligands
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Pyrroles
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Receptors, Estrogen
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Thiophenes