6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists

Wanying Sun, Lovji D. Cama, Elizabeth T. Birzin, Sudha Warrier, Louis Locco, Ralph Mosley, Milton L. Hammond, Susan P. Rohrer

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124 Citations (Scopus)

Abstract

A series of 6H-benzo[c]chromen-6-one and 6H-benzo[c]chromene derivatives were prepared, and the affinity and selectivity for ERα and ERβ was measured. Many of the analogs were found to be potent and selective ERβ agonists. Bis hydroxyl at positions 3 and 8 is essential for activity in a HTRF coactivator recruitment assay. Additional modifications at both phenyl rings led to compounds with ERβ < 10 nM potency and >100-fold selectivity over ERα.

Original languageEnglish
Pages (from-to)1468-1472
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number6
DOIs
Publication statusPublished - 15-03-2006
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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  • Cite this

    Sun, W., Cama, L. D., Birzin, E. T., Warrier, S., Locco, L., Mosley, R., Hammond, M. L., & Rohrer, S. P. (2006). 6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists. Bioorganic and Medicinal Chemistry Letters, 16(6), 1468-1472. https://doi.org/10.1016/j.bmcl.2005.12.057