引用本文:
罗稳, 李展, 翟洋洋, 谢松强, 王超杰. 萘酰亚胺多胺衍生物的合成及其抗肿瘤活性[J]. 应用化学,
2013, 30(3): 265-270.
doi:
10.3724/SP.J.1095.2013.20161
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
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
萘酰亚胺多胺衍生物的合成及其抗肿瘤活性
English
Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide
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.
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Key words:
- naphthalimide
- / DNA intercalator
- / antitumor
- / high content screening
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