Synthesis and biological evaluation of hydrazino-containing polyamine skeletons as drug delivery system

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., L1210, HeLa and B16) and the cellular entry of these polyamine conjugates via polyamine transporter was investigated on SPD- or DFMO-treated B16 cell line. Of these compounds, 6c show significant cytotoxicity on L1210, HeLa and B16 cell lines (IC50 value, 3.74 μmol/L, 5.66 μmol/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.