Abstract
Hydrogen bond effect plays a pivotal role in protein-ligand interaction and represents one of the fundamental bases in pharmaceutical design. To evaluate the influence of hydrogen bond interaction on the anti-breast cancer activity, fifteen dihydroartemisinin-isatin hybrids 7a-o with hydrogen bond donors at C-3 position of isatin moiety were designed, synthesized and evaluated for their antiproliferative activity against MCF-7, MDA-MB-231, MCF-7/ADR and MDA-MB-231/ADR breast cancer cell lines. The preliminary results illustrated that introduction of hydrogen bond donors especially thiosemicarbazide into C-3 position of isatin moiety was beneficial for the activity, and substituents at C-5 position of isatin fragment as well as the length of the carbon spacers between dihydroartemisinin and isatin moieties also have significant influence on the activity. The enriched structure-activity relationships may provide useful information for further rational design of the candidates with higher activity.
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