Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy

Nicole Lounsbury, George Mateo, Brielle Jones, Srinivas Papaiahgari, Rajash K. Thimmulappa, Christiana Teijaro, John Gordon, Kenneth Korzekwa, Min Ye, Graham Allaway, Magid Abou-Gharbia, Shyam Biswal, Wayne Childers

Research output: Contribution to journalArticlepeer-review

11 Scopus citations


Nrf2 activators represent a good drug target for designing agents to treat diseases associated with oxidative stress. Building upon previous work, we designed and prepared a series of heterocyclic chalcone-based Nrf2 activators with reduced lipophilicity and, in some cases, greater in vitro potency compared to the respective carbocyclic scaffold. These changes resulted in enhanced oral bioavailability and a superior pharmacodynamic effect in vivo.

Original languageEnglish (US)
Pages (from-to)5352-5359
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number17
StatePublished - Sep 1 2015


  • Bioavailability
  • Chalcone
  • Keap1
  • Nrf2
  • Solubility

ASJC Scopus subject areas

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


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