Solid-Phase synthesis and investigation of benzofurans as selective estrogen receptor modulators

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-α and ER-β, with some compounds having selectivity for ER-α. 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.