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Citation: LUO Wen, LI Zhan, ZHAI Yangyang, XIE Songqiang, WANG Chaojie. Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide[J]. Chinese Journal of Applied Chemistry, ;2013, 30(3): 265-270. doi: 10.3724/SP.J.1095.2013.20161 shu

Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide

a. Key Laboratory of Natural Medicine and Immuno-Engineering, He'nan University, Kaifeng 475004, China;
b. Institute of Chemical Bioogy, He'nan University, Kaifeng 475004, China

Received Date: 19 April 2012
Revised Date: 15 June 2012

A series of polyamine derivatives of naphthalimide(3a-3d) to be used as antitumor agents was synthesized.The biological and spectroscopic evaluations showed that compounds 3a-3d could used as DNA intercalators and had stronger cytotoxic activity and better selectivity than those of amonafide against cancer cells in vitro.The IC₅₀ for antiproliferative activity of compound 3b on four cancer cells were 7.80,5.08,9.78 and 9.27 μmol/L,respectively.High content screening(HCS) results revealed that the as-prepared compounds might produce cytotoxicity through apoptosis via mitochondrial pathway.
- naphthalimide,
- DNA intercalator,
- antitumor,
- high content screening
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