Synthesis Studies and the Evaluation of C6 Raloxifene Derivatives

被引：1

作者：

Williams, David R. ^{[1
]}

Taylor, Levin ^{[1
,3
]}

Miter, Gabriel A. ^{[1
]}

Sheiman, Johnathan L. ^{[1
]}

Wallace, Joseph M. ^{[2
]}

Allen, Matthew R. ^{[4
]}

Kohler, Rachel ^{[2
]}

Medeiros, Claudia ^{[2
]}

机构：

[1] Indiana Univ, Dept Chem, Bloomington, IN 47405 USA

[2] Indiana Univ Purdue Univ, Dept Biomed Engn, Indianapolis, IN 46202 USA

[3] Ment Performance Mat, Sistersville Site,10851 Energy Highway, Friendly, WV 26146 USA

[4] Indiana Univ Sch Med, Dept Anat Cell Biol & Physiol, Indianapolis, IN 46202 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2024年 / 15卷 / 06期

基金：

美国国家卫生研究院; 美国国家科学基金会;

关键词：

raloxifene derivatives; synthesis; methodology; estrogen binding affinity; bone properties; ESTROGEN-RECEPTOR MODULATORS; BONE-MINERAL DENSITY; ER-ALPHA; MECHANISM; SUBSTITUTION; COLLAGEN; SERIES;

D O I：

10.1021/acsmedchemlett.4c00078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Methodology is described for the synthesis of C-6 derivatives of raloxifene, a prescribed drug for the treatment and prevention of osteoporosis. Studies have explored the incorporation of electron-withdrawing substituents at C-6 of the benzothiophene core. Efficient processes are also examined to introduce hydrogen bond donor and acceptor functionality. Raloxifene derivatives are evaluated with in vitro testing to determine estrogen receptor (ER) binding affinity and gene expression in MC3T3 cells.

引用

页码：879 / 884

页数：6

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