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Current Topics in Medicinal Chemistry

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ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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Review Article

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

Author(s): Wei-Yun Guo, Shang-Ming-Zhu Zeng, Girdhar Singh Deora*, Qing-Shan Li* and Ban-Feng Ruan*

Volume 19, Issue 15, 2019

Page: [1318 - 1337] Pages: 20

DOI: 10.2174/1568026619666190619142504

Price: $65

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

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Graphical Abstract

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