A new 3-methoxybenzensulfonic acid 4-O-β-D-glucopyranoside (1), and ten known compounds (2–11) were isolated from the methanolic extract of the stems of Mallotus microcarpus. The cytotoxicity of the isolated compounds was evaluated by the MTT method. 3-Methoxybenzensulfonic acid 4-O-β-D-glucopyranoside (1) and methyl salicylate 2-rutinoside (5) showed strong cytotoxicity against EGFR-TKI-resistant human lung cancer A549 cells in comparison with camptothecin. Compound 1, leonuriside A (2), 3,4'-dihydroxypropiophenone 3-O-glucoside (6) and (1R,2S)-hovetrichoside A (10) inhibited the growth of human breast cancer MCF-7 cell line with IC50 values in the range of 0.48–1.78 μM. This is the first report on the chemical composition and cytotoxic activity of M. microcarpus.
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