Citation: Jian Hong Wang, Jun Jun Zhou, Song Qing Xie, Qian Li, Jin Zhao, Chao Jie Wang. Synthesis and biological evaluation of hydrazino-containing polyamine skeletons as drug delivery system[J]. Chinese Chemical Letters, ;2011, 22(1): 119-122. doi: 10.1016/j.cclet.2010.09.002 shu

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

Key Lab of Natural Medicinal and Immunotechnology of Henan Province, Henan University, Kaifeng 475004, China

Received Date: 26 March 2010

Fund Project: 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) and the Co-construction Projects of Henan University (No.SBGJ090518) for financial support of this research.

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 B 16 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.
- Polyamine conjugates,
- Polyamine transporter,
- Synthesis,
- Biological activity
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