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

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):2875-8. doi: 10.1016/s0960-894x(02)00613-3.
Roger A Smith  1 ,  Jinshan Chen ,  Mary M Mader ,  Ingo Muegge ,  Ulrike Moehler ,  Suresh Katti ,  Diana Marrero ,  William G Stirtan ,  Daniel R Weaver ,  Hong Xiao ,  William Carley
Affiliations
  • 1. Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA.
PMID: 12270167 DOI: 10.1016/s0960-894x(02)00613-3
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.