A new series of polyamine-toxic cargo conjugates was synthesized with aryl aldehydes conjugating to hydrazino-containing triamine skeletons. The in vitro cytotoxicity of target compounds was evaluated in several cancer cell lines （e.g., L I 210, HeLa and B16） and the cellular entry of these polyamine conjugates via polyamine transporter was investigated on SPD- or DFMO-treated B 16 cell line. Of these compounds, 6c show significant cytotoxicity on L 1210, HeLa and B 16 cell lines （IC50 value, 3.74 μmol/L, 5.66μmol/L and 4.04 μmol/L, respectively）. The polyamine transporter assay demonstrated the suitability of hydrazino-containing polyamine backbones for application as vectors in drug delivery systems.
Jian Hong Wang Jun Jun Zhou Song Qing Xie Qian Li Jin Zhao Chao Jie Wang
