期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 7, 页码 3502-3512出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm300168w
关键词
-
资金
- National Science Foundation of China [90913001]
With the aim of up-regulating antitumor efficacy and down-regulating adverse effects, three types of aromatic imide and diimides were designed to couple with different polyamines. The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell lines more potently than amonafide. 91, the most potent compound, was verified to efficiently induce apoptosis via a ROS mediated mitochondria] pathway in a preliminary mechanistic study. The comprehensive in vivo trials on three H22 tumor transplant models demonstrated that 9f improved the indexes in terms of inhibitive effect and lifespan extension and reduced the hematotoidcity which is one of main drawbacks of amonafide. More importantly, the obviously elevated ability in preventing lung cancer metastasis was observed, which increased the value of 9f as a promising lead compound. This work supported that the versatile function of polyamines may endow some intriguing biological features to the parent drugs.
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