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.

合成了一类新的通过多胺链末端的烷基化改性的多胺类似物，并通过¹ H NMR，¹³ C NMR，ESI-MS和元素分析确定了它们的结构。作为代表性化合物，3f通过MTT分析显示出广泛的抗癌作用。肿瘤异种移植模型和肺转移模型显示，化合物3f显着抑制了体内肿瘤的生长和转移，比参比药物阿莫那肽更强。分子机制表明化合物3f表现出抗增殖活性并诱导了活性氧（ROS）的产生，这导致了自噬的发生。化合物3f下调了MMP-9和β-catenin的表达是抑制迁移的原因。总之，体外和体内生物学评估证实了化合物3f是有效的抗癌剂。