Structure activity relationship for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene

被引：38

作者：

Overk, Cassia R.

Peng, Kuan-Wei

Asghodom, Rezene T.

Kastrati, Irida

Lantvit, Daniel D.

Qin, Zhihui

Frasor, Jonna

Bolton, Judy L.

Thatcher, Gregory R. J.

机构：

[1] Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612

[2] Department of Physiology and Biophysics, College of Medicine, University of Illinois at Chicago, Chicago

来源：

CHEMMEDCHEM | 2007年 / 2卷 / 10期

关键词：

D O I：

10.1002/cmdc.200700104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The search for the "ideal" selective estrogen receptor modulator (SERM) as a substitute for hormone replacement therapy (HRT) or use in cancer chemoprevention has focused on optimization of estrogen receptor (ER) ligand binding. Based on the clinical and preclinical benzothiophene SERMs, raloxifene and arzoxifene, a family of SERMs has been developed to modulate activity and oxidative lability. Antiestrogenic potency measured in human endometrial and breast cancer cells, and ER ligand binding data were correlated and seen to provide a guide to SERM design only when viewed in toto. The in vitro studies were extended to the juvenile rat model, in which the desired antiestrogenic profile and putative cardiovascular benefits of SERMs were observed.

引用

页码：1520 / 1526

页数：7