Williams, David R.Taylor, Levin, IVMiter, Gabriel A.Sheiman, Johnathan L.Wallace, Joseph M.Allen, Matthew R.Kohler, RachelMedeiros, Claudia2025-07-152025-07-152024-06-03Williams DR, Taylor L 4th, Miter GA, et al. Synthesis Studies and the Evaluation of C6 Raloxifene Derivatives. ACS Med Chem Lett. 2024;15(6):879-884. Published 2024 Jun 3. doi:10.1021/acsmedchemlett.4c00078https://hdl.handle.net/1805/49438Methodology 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.en-USPublisher PolicyRaloxifene derivativesSynthesisMethodologyEstrogen binding affinityBone propertiesArticle