WHN-11

WHN-11 is a novel semi-synthetic C-10 substituted amino-artemisinin derivative, specifically characterized as a 4'-trifluoromethylarylurea piperazinyl derivative. It exhibits potent anti-cancer and anti-cancer stem cell activity, particularly against triple-negative breast cancer (TNBC) cell lines. Mechanistically, WHN-11 disrupts mitochondrial integrity by inducing depolarization and fission, which leads to the suppression of the anti-apoptotic protein B-cell lymphoma extra-large (Bcl-xL) and a reduction in ATP synthesis. Furthermore, it interferes with protein homeostasis by increasing the proteasome-mediated turnover of ubiquitinated proteins and induces cellular stress responses, including autophagy and apoptosis. Notably, the cytotoxic effects of WHN-11 appear to be independent of substantial reactive oxygen species (ROS) production, distinguishing it from other artemisinin derivatives.

Other names

4'-trifluoromethylarylurea piperazinyl amino-artemisinin derivative