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Updated: Jan 23, 2026

Imaging of Estrogen Receptor-α in Rat Pial Arterioles using a Digital Immunofluorescent Microscope
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Imaging of Estrogen Receptor-α in Rat Pial Arterioles using a Digital Immunofluorescent Microscope

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Estrogen Receptor α (ERα)-targeting Compounds and Derivatives: Recent Advances in Structural Modification and

Wei-Yun Guo1, Shang-Ming-Zhu Zeng1, Girdhar Singh Deora2

  • 1School of Food and Biological Engineering, Hefei University of Technology, Hefei, 230009, China.

Current Topics in Medicinal Chemistry
|June 20, 2019
PubMed

Insights

This review explores recent advances in breast cancer treatment, focusing on novel analogs and derivatives for hormone therapies like SERMs, SERDs, and AIs. It addresses the need for improved treatments due to resistance and side effects of current options.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Breast cancer is a leading cause of female cancer deaths globally.
  • Current hormone therapies (SERMs, SERDs, AIs) face challenges like resistance and side effects.
  • Improved therapeutic strategies are crucial for better patient outcomes.

Purpose of the Study:

  • To review recent literature (past five years) on breast cancer hormone therapy.
  • To focus on the isolation and synthesis of novel analogs and derivatives.
  • To identify potential new treatments overcoming current therapy limitations.

Main Methods:

  • Comprehensive literature search of scientific databases.
  • Analysis of studies on the synthesis and biological activity of estrogen receptor modulators.
  • Review of research on analogs and derivatives of SERMs, SERDs, and AIs.

Main Results:

  • Identification of diverse synthetic strategies for novel compounds.
  • Evaluation of the efficacy and safety profiles of new analogs and derivatives.
  • Emerging trends in developing targeted therapies for hormone-dependent breast cancer.

Conclusions:

  • Significant progress has been made in synthesizing novel breast cancer therapeutic agents.
  • New analogs and derivatives show promise in overcoming resistance and reducing side effects.
  • Continued research into these compounds is vital for advancing breast cancer treatment.
Keywords:
AnalogsBioactivityBreast cancerDerivativesEstrogen receptor αStructure-activity relationship.

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