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

Wei-Yun Guo; Shang-Ming-Zhu Zeng; Girdhar Singh Deora; Qing-Shan Li; Ban-Feng Ruan

doi:10.2174/1568026619666190619142504

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

Curr Top Med Chem. 2019;19(15):1318-1337. doi: 10.2174/1568026619666190619142504.

Authors

Wei-Yun Guo¹, Shang-Ming-Zhu Zeng¹, Girdhar Singh Deora², Qing-Shan Li¹, Ban-Feng Ruan¹

Affiliations

¹ School of Food and Biological Engineering, Hefei University of Technology, Hefei, 230009, China.
² Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

PMID: 31215379
DOI: 10.2174/1568026619666190619142504

Abstract

Breast cancer is the most common cancer suffered by female, and the second highest cause of cancer-related death among women worldwide. At present, hormone therapy is still the main treatment route and can be divided into three main categories: selective estrogen receptor modulators (SERMs), selective estrogen receptor downregulators (SERDs), and aromatase inhibitors (AIs). However, breast cancer is difficult to cure even after several rounds of anti-estrogen therapy and most drugs have serious side-effects. Here, we review the literature published over the past five years regarding the isolation and synthesis of analogs and their derivatives.

Keywords: Analogs; Bioactivity; Breast cancer; Derivatives; Estrogen receptor α; Structure-activity relationship..

Publication types

Review

MeSH terms

Animals
Antineoplastic Agents / chemistry
Antineoplastic Agents / isolation & purification
Antineoplastic Agents / pharmacology*
Aromatase Inhibitors / chemistry
Aromatase Inhibitors / isolation & purification
Aromatase Inhibitors / pharmacology*
Breast Neoplasms / drug therapy*
Breast Neoplasms / metabolism
Breast Neoplasms / pathology
Cell Proliferation / drug effects
Drug Screening Assays, Antitumor
Estrogen Receptor Antagonists / chemistry
Estrogen Receptor Antagonists / isolation & purification
Estrogen Receptor Antagonists / pharmacology*
Estrogen Receptor Modulators / chemistry
Estrogen Receptor Modulators / isolation & purification
Estrogen Receptor Modulators / pharmacology*
Estrogen Receptor alpha / antagonists & inhibitors*
Estrogen Receptor alpha / metabolism
Female
Humans
Molecular Structure

Substances

Antineoplastic Agents
Aromatase Inhibitors
Estrogen Receptor Antagonists
Estrogen Receptor Modulators
Estrogen Receptor alpha