Synthesis Studies and the Evaluation of C Raloxifene Derivatives

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2024 Jun 19

PMID 38894928

Authors

David R Williams

Levin Taylor 4th

Gabriel A Miter

Johnathan L Sheiman

Joseph M Wallace

Matthew R Allen

Rachel Kohler

Claudia Medeiros

Affiliations

Soon will be listed here.

Abstract

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

Citing Articles

Effects of novel raloxifene analogs alone or in combination with mechanical loading in the Col1a2 murine model of osteogenesis imperfecta.

Kohler R, Creecy A, Williams D, Allen M, Wallace J Bone. 2023; 179:116970.

PMID: 37977416 PMC: 10843597. DOI: 10.1016/j.bone.2023.116970.

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