Given the reported cytotoxicity of phthaloylaminoethyltriphenylphosphonium bromide 2a in the P-388 cell line, we have developed new [2-(phthaloylamino)alkyl]phosphonium derivatives 2b-e and evaluated their cytotoxic activity. These compounds have been synthetized from N,N-phthaloylaminoalcohols and triphenylphosphonium hydrobromide via a one-pot reaction. 2a was found inactive in the K562 cell line, but 2c-e exhibited a cytotoxic activity with IC50 values about 1 microM.