Recent advances in the synthesis of raloxifene: A selective estrogen receptor modulator

被引：57

作者：

Dadiboyena, Sureshbabu ^{[1
,2
]}

机构：

[1] Torrey Pines Inst Mol Studies, Port St Lucie, FL 34987 USA

[2] Mississippi State Univ, Mississippi State, MS 39762 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 51卷

关键词：

Raloxifene; Evista (R); Estrogen Receptors; Heterocycles; Benzothiophenes; SERM; Steroids; THIANAPHTHEN-2-ONE CHEMISTRY; EFFICIENT SYNTHESIS; BINDING AFFINITIES; HIGHLY POTENT; LIGANDS; DERIVATIVES; ANALOGS; SUBSTITUTION; CANCER; ALPHA;

D O I：

10.1016/j.ejmech.2012.02.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Estrogens are a group of steroids that exert important effects on reproductive and many nonreproductive tissues. Selective estrogen receptor modulators (SERM) are a class of therapeutic agents widely prescribed for the treatment and prevention of breast cancer, osteoporosis, and postmenopausal symptoms. Raloxifene, an example of oral SERM is prescribed primarily for the treatment and prevention of postmenopausal disorders in woman. The current review provides an outline of practical methodologies used to access benzothiophenyl scaffolds of raloxifene and relevant structural analogs. The contents are discussed in five sections: (a) synthesis of raloxifene, (b) organometallic analogs, (c) radiolabelled analogs, (d) constrained raloxifene analogs, and (e) other oxygen, sulfur, and nitrogen based raloxifene analogs. In addition to the synthesis, biological activity of a few synthetic analogs has been discussed. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：17 / 34

页数：18

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