Synthesis, cytotoxicity and apoptosis of naphthalimide polyamine conjugates as antitumor agents

被引：64

作者：

Tian, Zhi-yong ^{[2
,3
]}

Xie, Song-qiang ^{[2
]}

Du, Yao-wu ^{[4
]}

Ma, Yuan-fang ^{[4
]}

Zhao, Jin ^{[2
]}

Gao, Wen-yuan ^{[3
]}

Wang, Chao-jie ^{[1
,2
]}

机构：

[1] Henan Univ, Dept Chem, Kaifeng 475001, Henan, Peoples R China

[2] Henan Univ, Inst Nat Prod & Med Chem, Kaifeng 475001, Peoples R China

[3] Tianjin Univ, Coll Pharm, Tianjin 300072, Peoples R China

[4] Henan Univ, Coll Med, Kaifeng 475001, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 01期

基金：

美国国家科学基金会;

关键词：

Naphthalimide; Polyamine conjugate; Synthesis; Cytotoxicity; Apoptosis; BIOLOGICAL EVALUATION; MOLECULAR REQUIREMENTS; SELECTIVE DELIVERY; CELLS; AMONAFIDE; CANCER; DERIVATIVES; TRANSPORT; SPERMINE; ANALOG;

D O I：

10.1016/j.ejmech.2008.02.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several naphthalimide polyamine conjugates were synthesized and evaluated for in vitro cytotoxicity against human leukemia K562, murine melanoma B16, Chinese hamster ovary CHO cell lines. Both triamine moieties and the length of spacers were crucial in elevating the potency of 1,8-naphthalimide. The typical compounds 5a and 5d exhibited excellent cell selectivity to cancer cells through the human hepatoma BEL-7402 and human normal hepatocyte QSG-7701 screens. In addition, 5d could disturb the cell cycle in B16 cells. The research on caspase activity and cytochrome c indicated that 5d could induce B16 cell apoptosis via both the mitochondrial and membrane death receptor pathways, and the Bcl-2 family numbers were involved in the control of apoptosis. (C) 2008 Elsevier Masson SAS. All fights reserved.

引用

页码：393 / 399

页数：7

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