This is an archive of papers published by the staff and faculty of Fox Chase Cancer Center. For questions about content, please contact Talbot Research Library
Last updated on
Lounsbury N , Mateo G , Jones B , Papaiahgari S , Thimmulappa RK , Teijaro C , Gordon J , Korzekwa K , Ye M , Allaway G , Abou-Gharbia M , Biswal S , Childers W Jr
Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy
Bioorg Med Chem. 2015 Sep 1;23(17) :5352-9
PMID: 26278028 URL: https://www.ncbi.nlm.nih.gov/pubmed/26278028
AbstractNrf2 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.
NotesLounsbury, Nicole Mateo, George Jones, Brielle Papaiahgari, Srinivas Thimmulappa, Rajash K Teijaro, Christiana Gordon, John Korzekwa, Kenneth Ye, Min Allaway, Graham Abou-Gharbia, Magid Biswal, Shyam Childers, Wayne Jr Research Support, Non-U.S. Gov't England Bioorg Med Chem. 2015 Sep 1;23(17):5352-9. doi: 10.1016/j.bmc.2015.07.056. Epub 2015 Jul 29.