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Li, Jinghua; Tian, Runguo; Ge, Chaochao; Chen, Ying; liu, Xiaodan; Wang, Yuxia; Yang, Yacheng; Luo, Wen; Dai, Fujun; Wang, Senzhen; Chen, Shuai; Xie, Songqiang; Wang, Chaojie
Journal of medicinal chemistry, 08/2018, Volume: 61, Issue: 15Journal Article
Polyamine derivatives have a promising prospect in dealing with disseminated tumor cells, a major obstacle in cancer therapy. To develop a bifunctional polyamine derivative that can serve as a fluorescent probe and an antimetastatic agent, three kinds of polyamine conjugates with benzocdindol-2(1H)-one as a scaffold were designed and synthesized. Compound 5e was selected as a lead by in vitro screening. Two animal models demonstrated that 5e inhibited pulmonary metastasis and tumor growth. As a fluorescent probe, 5e might partially enter cells via a polyamine transporter and subsequently localize in the lysosome. Mechanistic investigations demonstrated the interdependence of 5e-triggered apoptosis and autophagy. Compound 5e modulated the expression of LC3-II, p62, cathepsins, and the expression of capases 3, caspase 8, Bcl-2, and p53. The SSAT-mediated Akt/β-catenin pathways were also inhibited by 5e. The dual features of 5e make it a worthwhile lead compound for further structural optimization.
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