Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. They were also potent agonists in bone tissue.
Yang
Chunhao
C
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. chyang@mail.shcnc.ac.cn
Xu
Guangyu
G
Li
Jia
J
Wu
Xihan
X
Liu
Bo
B
Yan
Xueming
X
Wang
Mingwei
M
Xie
Yuyuan
Y
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D015519:Bone Density / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D047628:Estrogen Receptor alpha / Q000819:agonists* / Q000037:antagonists & inhibitors; D005260:Female; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis*; D020849:Raloxifene Hydrochloride / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry*; D014599:Uterus / Q000187:drug effects
D047628:Estrogen Receptor alpha; D008024:Ligands; D010879:Piperazines; D020845:Selective Estrogen Receptor Modulators; D013876:Thiophenes; C088015:benzothiophene; D020849:Raloxifene Hydrochloride