This paper describes the cytotoxic and antitumoral activities of kaempferol 3-O-(6”-O-E-pcoumaroyl)-β-D-glucopyranoside (tiliroside), kaempferol 3,7-di-O-α-L-rhamnoside (dhiramnoside) and of the mixture of sitosteryl-3-O-β-D-glucopyranoside and stigmasteryl-3-O-β-D-glucopyranoside (GM) isolated of the Herissantia crispa. The compounds did not present cytotoxic activity against NCI-H292, HEp-2 and KB cells. In vivo, dhiramnoside did not present significant inhibitory activity of the growth of sarcoma 180 when compared with the control group; however, tiliroside and GM-treated animals showed a high inhibition rate in the growth of the tumor. Tiliroside inhibits significantly the growth of the carcinoma of Ehrlich. In conclusion, tiliroside exhibited promising antitumor effects without an expressive toxicity.