LAUSR

The synthesized 11 artemisinin‐isatin hybrids 5a–c and 6a–h tethered via ethylene linker were assessed for their in vitro antiproliferative activity against A549 and H1299 nonsmall‐cell lung cancer cell lines as well as their cytotoxicity towards BEAS‐2B human normal lung epithelial cells. The preliminary results showed that hybrids 5a–c and 6a–h did not show any cytotoxicity (IC50: >100 µM) on BEAS‐2B cells, and also possessed potential activity (IC50: 6.99–76.49 µM) against A549 and H1299 lung cancer cell lines. The representative hybrid 6c (IC50: 6.99 and 7.57 µM) was far more potent than artemisinin (IC50: >100 µM) and dihydroartemisinin (IC50: >100 µM), and was slightly less active than doxorubicin (IC50: 4.14 and 2.77 µM). Moreover, hybrid 6c also exhibited an excellent safety profile and good selectivity with SI values of >13.21. Therefore, hybrid 6c could serve as a promising candidate for further in vivo evaluations.