Aza analogues of equol: Novel ligands for estrogen receptor β

3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERα and ERβ. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: an...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2007-09, Vol.15 (17), p.5828-5836
Hauptverfasser:	Chen, Wuhong, Lin, Zhaohu, Ning, Mengmeng, Yang, Chunhao, Yan, Xueming, Xie, Yuyuan, Shen, Xu, Wang, Ming-Wei
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Phenyl-tetrahydroquinoline Animals Aza Compounds - chemical synthesis Aza Compounds - chemistry Aza Compounds - pharmacology Biological and medical sciences Bone Density Equol ERβ Estrogen Receptor alpha - metabolism Estrogen Receptor beta - metabolism Female Hormones. Endocrine system Humans Isoflavones - chemical synthesis Isoflavones - chemistry Isoflavones - pharmacology Ligands Medical sciences Molecular Structure Pharmacology. Drug treatments Rats Structure-Activity Relationship Uterus - drug effects
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Zusammenfassung:	3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERα and ERβ. 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 ERα and agonists for ERβ in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2007.05.071