The potential role of the 5,6-dihydropyridin-2(1<i>H</i>)-one unit of piperlongumine on the anticancer activity
Wen‐Wen Mu, Peng‐Xiao Li, Guoyun Liu, Jie Yang, Guoyun Liu
Abstract
)-one unit, a potent pharmacophore in enhancing the antiproliferative activities of PL, could react with cysteamine and lead to ROS generation, and then bring about the occurrence of ROS-induced downstream events, followed by cell cycle arrest and apoptosis. This work suggests that introducing a lactam unit containing Michael acceptors may be a potent strategy to enhancing the anticancer activity of drugs.
Topics & Concepts
PharmacophoreCytotoxicityChemistryApoptosisStereochemistryCombinatorial chemistryPharmacologyIn vitroBiochemistryBiologyPiperaceae Chemical and Biological StudiesGinger and Zingiberaceae researchPhenothiazines and Benzothiazines Synthesis and Activities