New alkaloid-containing derivatives of the sesquiterpene lactones arglabin, grosshemin, 3,4β-epoxyarglabin, argolide, and parthenolide were prepared for the first time. Their structures were studied using PMR, 13C NMR, and mass spectra and an X-ray crystal structure analysis. Chemo- and regioselective reactions of the sesquiterpene lactones and alkaloids were observed. The synthesized compounds exhibited anthelmintic and hepatoprotective activity and cytotoxicity. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.