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

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Tian ZY,Xie SQ,Du YW,Ma YF,Zhao J,Gao WY,Wang CJ

doi

10.1016/j.ejmech.2008.02.044

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

393-9

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00127-X

journal_volume

44

pub_type

杂志文章

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