A less lipophilic non-sesquiterpenoid antitumor constituent, methyl caffeate, along with D-fructose, was isolated from the aqueous methanol extract of the dried whole plant of Gaillardia pulchella. Among forty-three synthetic catechol analogues related to methyl caffeate tested for antitumor activity against Sarcoma 180 in mice, acetates of methyl catecholylpropionoid type showed stronger activity than the corresponding catechuic acid and catechualdehyde derivatives as well as simple benzaldehyde (so-called vidrol). None of the catecholic and related compounds tested showed significant antimicrobial activity in vitro.