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Synthesis Studies and the Evaluation of C6 Raloxifene Derivatives
David R Williams1, Levin Taylor1, Gabriel A Miter1
1Department of Chemistry, Indiana University, Bloomington, Indiana 47405, United States.
Abstract:
Methodology is described for the synthesis of C6 derivatives of raloxifene, a prescribed drug for the treatment and prevention of osteoporosis. Studies have explored the incorporation of electron-withdrawing substituents at C6 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.
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