New derivatives of 1,4-dideoxy-1,4-imino-D-ribitol have been prepared and evaluated for their cytotoxicity on solid and haematological malignancies. 1,4-Dideoxy-5-O-[(9Z)-octadec-9-en-1-yl]-1,4-imino-Dribitol (13, IC50 similar to 2 mu M) and its C-18-analogues (IC50 < 10 mu M) are cytotoxic toward SKBR3 (breast cancer) cells. 13 also inhibits (IC50 similar to 8 mu M) growth of JURKAT cells. (C) 2011 Published by Elsevier Ltd.