Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs
Graphical abstract
Chromanes I were discovered as SERAMs (Selective Estrogen Receptor Alpha Modulators) with the potential for the treatment of osteoporosis and cancer.
Section snippets
Acknowledgements
The authors would like to thank Dr. Mats Carlquist and his colleagues at Karo-Bio for providing protein samples for X-ray crystallography analysis. Use of the Advanced Photon Source beamline 17-ID was supported by the companies of the Industrial Macromolecular Crystallography Association through a contract with Illinois Institute of Technology.
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2017, Bioorganic and Medicinal Chemistry LettersCitation Excerpt :The coumarin scaffold has been known to medicinal chemists for about 50 years for its antagonistic properties against the ER.15,16 In recent years, 7-hydroxycoumarins, 7-hydroxychromenes and 7-hydroxychromanes, have been reported as selective ER ligands or modulators (SERMs) by many academic groups and pharmaceutical companies.17–21 SP500263 (3), a coumarin-based SERM, binds with high affinity to ERα and potently inhibits estrogen-dependent MCF-7 proliferation with similar IC50 value to tamoxifen (Fig. 1).22
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