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Synthesis and biological evaluation of novel alkylated polyamine analogues as potential anticancer agents.

Abstract：

:A new class of polyamine analogues modified by alkylation at the terminal of the polyamine chain has been synthesized and their structures were determined by 1H NMR, 13C NMR, ESI-MS and elemental analysis. As the representative compound, 3f displayed a broad spectrum of anti-cancer effects by MTT assays. Tumor xenograft model and pulmonary metastasis model showed that compound 3f significantly suppressed tumor growth and metastasis in vivo, which was more stronger than the reference drug amonafide. Molecular mechanisms indicated that compound 3f exhibited antiproliferative activities and induced the generation of reactive oxygen species (ROS), which resulted in the occurrence of autophagy. The downregulated expression of MMP-9 and β-catenin by compound 3f accounted for the inhibition of migration. Taken altogether, the in vitro and in vivo biological evaluations corroborated compound 3f to be an effective anticancer agent.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Li M,Wang Y,Ge C,Chang L,Wang C,Tian Z,Wang S,Dai F,Zhao L,Xie S

doi

10.1016/j.ejmech.2017.10.069

subject

Has Abstract

pub_date

2018-01-01 00:00:00

pages

1732-1743

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30871-1

journal_volume

143

pub_type

杂志文章

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