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Twelve cinnamoyl glucoside derivatives were prepared by glycosylation of glucosyl trichloroacetimidate and cinnamic acid derivatives, followed by dechloroacetylation with a pyridine/H2O mixture. Their structures were characterized by 1H and 13C NMR, as well as mass analysis. All the products were tested for their antiproliferation activities against murine melanoma B16-F10 cell line. Compounds 4e-4j were able to inhibit the proliferation of murine melanoma B16-F10 cell line with IC50 values of 17.38 ± 0.07, 9.87 ± 0.09, 9.69 ± 0.12, 29.42 ± 0.04, 32.95 ± 0.08, 25.68 ± 0.09 μM, respectively.
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•Twelve cinnamoyl glucoside derivatives were prepared in good yields under mild, concise reaction conditions.•Ten were new compounds and synthesized for the first time.•All were tested for antiproliferation activities against B16 cell line for the first time.•Six of them (4e–4j) exhibited moderate to good antiproliferation activities.