Review Article

Antitumor Activity of Artemisinin and Its Derivatives: From a Well-Known Antimalarial Agent to a Potential Anticancer Drug

Table 1

Factors that may influence artemisinins response in cancer cells.

SystemFactor/characteristic

Cancer cellProliferating activity
Expression of transferrin receptors
Accumulation levels of iron
Levels of gene expression (i.e., proapoptotic and antiapoptotic genes)
Shifting hallmarks
Overexpression of potential molecular targets in some tumors
Cellular dependence on redox balance
Expression of antioxidant enzymes
Expression of estrogen receptors in breast cancer cells

Artemisinin compoundDose and time of exposure
Chemical structure: number of trioxane rings, for example, dimeric compounds can be up to >1000 fold-more potent than monomeric artemisinins [61]
In dimeric endoperoxides: nature and stereochemistry of the linker
In novel compounds, electrophilic substitutions in the ring or those conferring lipophilicity. Boat/chair conformation