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

Research output: Contribution to journalArticle

113 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

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Benzopyrans
Hydroxyl Radical
Assays
Derivatives
6H-benzo(c)chromen-6-one

All Science Journal Classification (ASJC) codes

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

Cite this

Sun, W., Cama, L. D., Birzin, E. T., Warrier, S., Locco, L., Mosley, R., ... 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
Sun, Wanying ; Cama, Lovji D. ; Birzin, Elizabeth T. ; Warrier, Sudha ; Locco, Louis ; Mosley, Ralph ; Hammond, Milton L. ; Rohrer, Susan P. / 6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 6. pp. 1468-1472.
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Sun, W, Cama, LD, Birzin, ET, Warrier, S, Locco, L, Mosley, R, Hammond, ML & Rohrer, SP 2006, '6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 6, pp. 1468-1472. https://doi.org/10.1016/j.bmcl.2005.12.057

6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists. / Sun, Wanying; Cama, Lovji D.; Birzin, Elizabeth T.; Warrier, Sudha; Locco, Louis; Mosley, Ralph; Hammond, Milton L.; Rohrer, Susan P.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 6, 15.03.2006, p. 1468-1472.

Research output: Contribution to journalArticle

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AU - Cama, Lovji D.

AU - Birzin, Elizabeth T.

AU - Warrier, Sudha

AU - Locco, Louis

AU - Mosley, Ralph

AU - Hammond, Milton L.

AU - Rohrer, Susan P.

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