Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators |
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| Authors: | Smith Roger A Chen Jinshan Mader Mary M Muegge Ingo Moehler Ulrike Katti Suresh Marrero Diana Stirtan William G Weaver Daniel R Xiao Hong Carley William |
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| Institution: | Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA. |
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| Abstract: | A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay. |
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