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

Bioorg Med Chem. 2018 May 1;26(8):1638-1642. doi: 10.1016/j.bmc.2018.02.010. Epub 2018 Feb 9.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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