2. Academic Validation
  3. Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021)

Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021)

  • Eur J Med Chem. 2022 Feb 15:230:114119. doi: 10.1016/j.ejmech.2022.114119.
Youquan Xie 1,  Yucheng Tian 1,  Yuming Zhang 1,  Zhisheng Zhang 1,  Rui Chen 1,  Mian Li 1,  Jiawei Tang 1,  Jinlei Bian 1,  Zhiyu Li 2,  Xi Xu 3
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, PR China.
  • 2 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, PR China. Electronic address: zhiyuli@cpu.edu.cn.
  • 3 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, PR China. Electronic address: xuxi@cpu.edu.cn.
PMID: 35063736 DOI: 10.1016/j.ejmech.2022.114119
Abstract

Osteoporosis is a common disease in which the risk of fracture increases due to decreased bone mass and qualitative skeletal changes. Selective Androgen Receptor modulators (SARMs) are agonists with tissue selectivity, which act as partial or weak Androgen Receptor (AR) agonists in androgenic tissues, but mainly as complete AR agonists in synthetic metabolic tissues. In the recent 20 years, many scaffolds of SARMs have been reported, among which several molecules are promising and are undergoing clinical trial evaluation. However, it is still a challenge to discover SARMs with high activity and reduced side effects. In this review, not only are structure of SARMs reported in the literatures systematically collected and classified but also the structure-activity relationships (SAR) are systematically summarized. Furthermore, the advances in SARMs as potential treatment for osteoporosis are also updated.

Keywords

Osteoporosis; Selective androgen receptor modulators; Structure-activity relationships.

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