Affiliation:
1. School of Pharmacy Guizhou University of Traditional Chinese Medicine 550025 Guiyang Guizhou PR China
Abstract
AbstractA series of novel pentanoate tethered artemisinin‐isatin hybrids 6 a–d and 7 a–m were synthesized and evaluated their activity against CCRF‐CEM, K562 and K562/ADR leukemia cell lines as well as normal human peripheral blood mononuclear cells (PBMCs) by MTT assay. In particular, hybrid 7 b (IC50: 2.30 and 2.77 μM) exhibited highest activity against CCRF‐CEM and K562 cells, and the activity was not inferior to these of adriamycin (IC50: 4.89 μM) and vorinostat (IC50: 3.83 μM) against K562 cells, whereas hybrid 7 g (IC50: 0.62 μM) was more potent than adriamycin (IC50: 4.89 μM) and vorinostat (IC50: 3.83 μM) against K562/ADR cells. Moreover, the two hybrids (IC50: >100 μM) displayed non‐cytotoxicity towards normal PBMCs cells, and the selectivity index values were >11.02, indicating their excellent selectivity and safety profiles. Thus, hybrids 7 b and 7 g could act as potential anti‐leukemic candidates and were worthy of further preclinical evaluations.