Synthesis and cytotoxic activity of novel dihydroartemisinin-nonsteroidal anti-inflammatory drug conjugates

In this study, a series of novel dihydroartemisinin-nonsteroidal anti-inflammatory drug conjugates was designed and synthesised. The cytotoxic effects of these compounds against human leukemic K562 and multidrug-resistant K562/ADR cell lines were evaluated using the CCK-8 assay in vitro. Most hybrids exhibited higher anticancer activities than dihydroartemisinin. Among them, compound KL-7 demonstrated the highest potency, with IC50 values of 0.11 ± 0.01 μM and 0.34 ± 0.02 μM against K562 and K562/ADR cells, respectively. Moreover, KL-7 showed selectivity comparable to that of the positive drug etoposide. Further analysis revealed that KL-7 significantly induced apoptosis in K562/ADR cells. The drug-likeness of KL-7 was also predicted.