Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.

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.

• Authors: Ryo Eto, Takashi Misawa, Tomomi Noguchi-Yachide, Nobumichi Ohoka, Masaaki Kurihara, Mikihiko Naito, Masakazu Tanaka, Yosuke Demizu
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 26 Issue 8 Pg. 1638-1642 (05 01 2018) ISSN: 1464-3391 [Electronic] England
• PMID: 29525335 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2018 Elsevier Ltd. All rights reserved.

Chemical References

• Estrogen Receptor Antagonists
• Heptanes
• Indoles
• Ligands
• Pyrroles
• Receptors, Estrogen
• Thiophenes

Topics

• Dose-Response Relationship, Drug
• Drug Design
• Estrogen Receptor Antagonists (chemical synthesis, chemistry, pharmacology)
• Heptanes (chemical synthesis, chemistry, pharmacology)
• Humans
• Indoles (chemical synthesis, chemistry, pharmacology)
• Ligands
• MCF-7 Cells
• Models, Molecular
• Molecular Structure
• Pyrroles (chemical synthesis, chemistry, pharmacology)
• Receptors, Estrogen (antagonists & inhibitors, metabolism)
• Structure-Activity Relationship
• Thiophenes (chemical synthesis, chemistry, pharmacology)
• Tumor Cells, Cultured