Aza analogues of equol: Novel ligands for estrogen receptor beta

作者：Chen, Wuhong; Lin, Zhaohu; Ning, Mengmeng; Yang, Chunhao^*; Yan, Xueming; Xie, Yuyuan; Shen, Xu; Wang, Ming-Wei

来源：Bioorganic & Medicinal Chemistry, 2007, 15(17): 5828-5836.

DOI：10.1016/j.bmc.2007.05.071

• 3-phenyl-tetrahydroquinoline
• ER beta
• equol

3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ER alpha and ER beta. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: antagonists for ERa and agonists for ER beta in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.

• 出版日期2007-9-1
• 单位国家新药筛选中心; 华东理工大学; 中国科学院; 中国科学院上海生命科学研究院; 中国科学院上海药物研究所; 新药研究国家重点实验室