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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
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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.
Lounsbury, 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.