Antiproliferation and apoptosis induced by C-glycosides in human leukemia cancer cells

A large series of alkyl C-glycosides was synthesized from d-glucal or d-galactal. These compounds were screened against the human promyelocytic leukemia cell line (HL60), showing significant activity and apoptosis. Up to 13 C-glucopyranosides, but no C-galacto- or C-mannopyranosides, exhibited inhibitory concentrations (IC50 values) below 20 μM, five of them in the range 4–8 μM. Preliminary structure–activity relationships were established.