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

[Display omitted] 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 ar...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2018-05, Vol.26 (8), p.1638-1642
Main Authors: Eto, Ryo, Misawa, Takashi, Noguchi-Yachide, Tomomi, Ohoka, Nobumichi, Kurihara, Masaaki, Naito, Mikihiko, Tanaka, Masakazu, Demizu, Yosuke
Format: Article
Language:English
Subjects:
Antagonist
Estrogen receptor
Heterocycles
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Summary:[Display omitted] 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2018.02.010