Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide

doi:10.3724/SP.J.1095.2012.20161

Chinese Journal of Applied Chemistry

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Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide

LUO Wen¹, LI Zhan¹, ZHAI Yangyang¹, XIE Songqiang^2*, WANG Chaojie^1*

(1.Key Laboratory of Natural Medicine and Immuno-Engineering;2.Institute of Chemical Bioogy,He′nan University,Kaifeng 475004,China)

Received:2012-04-19 Revised:2012-06-14 Published:2013-03-10 Online:2013-03-10
Contact: wang Chaojie

Abstract

Abstract: 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.

Key words: Naphthalimide, DNA intercalator, antitumor, High Content Screening

CLC Number:

O622.6

LUO Wen1, LI Zhan1, ZHAI Yangyang1, XIE Songqiang2*, WANG Chaojie1*. Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2012.20161.

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Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide

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