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

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)1318-1337
Number of pages20
JournalCurrent Topics in Medicinal Chemistry
Issue number15
Publication statusPublished - 1 Jan 2019


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

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