A series of four novel hydrazine-modified diamine conjugates (7a-b, 8a-b) were synthesized and evaluated for cytotoxicityagainst Melanoma B 16, α-difluoromethylornithine (DFMO)-treated B 16, spermidine (SPD)-treated B 16, Mouse leukemia L 1210and Hela cell lines. Both the DFMO-B 16 and SPD-B 16 experiments indicated that conjugates 7a-b and 8a-b could recognize thepolyamine transporter (PAT) and enter the cells in part or in whole via PAT, although they were not as efficient as the reference, 9-anthracenemethyl homospermidine (1).