From the natural product 4-(4'-O-acetyl-a-L-rhamnosyloxy) benzylisothiocyanate (1), isolated from the flowers of Moringa oleifera Lam (Moringaceae), four new semisynthetic derivatives, N-[4-(4'-O-acetyl-alpha-L-rhamnosyloxy) benzyl]-2-(pyridinil-4-carbonil) hydrazine-1-carbothioamide (3), 4-(4'-O-acetyl-2', 3'-dimesyloxy-alpha-L-rhamnosyloxy) benzylisothiocyanate (4), N-[(4'-O-acetyl-alpha-Lrhamnosyloxy) benzyl] hydrazinecarbothioamide (5), 4-[4'-O-acetyl-2', 3'-O-bis(decanoiloxy)-alpha-L-rhamnosyloxy] benzylisothiocianate (6), and the known compound 4-(2', 3', 4'-O-triacetyl-alpha-L-rhamnosyloxy) benzylisothiocyanate (2), were obtained. All compounds were tested for their cytotoxicity against the tumor cell lines SF-295, HL-60, HCT-116 e PC-3. The natural product 1 and the semisynthetic derivatives 2 and 4 were the most active compounds (IC50 from 16.0 to 3.7 mu mol L-1) against all tumor cell lines.