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 cance...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.展开更多
基金The authors gratefully thank the National Natural Science Foundation of China(Nos.20872027 and 90913001)the Key Scientific and Technological Projects of Henan province(Nos.092102310025,102102210075,and 102102310195)the Co-construction Projects of Henan University(No.SBGJ090518)for financial support of this research
文摘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.
