The synthesis and molecular recognization of the polyamine transporter of hydrazine-modified diamine conjugates

Abstract

A series of four novel hydrazine-modified diamine conjugates ( 7a- b, 8a- b) were synthesized and evaluated for cytotoxicity against Melanoma B16, α-difluoromethylornithine (DFMO)-treated B16, spermidine (SPD)-treated B16, Mouse leukemia L1210 and Hela cell lines. Both the DFMO-B16 and SPD-B16 experiments indicated that conjugates 7a- b and 8a- b could recognize the polyamine 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).