Platinum(IV) complexes conjugated with phenstatin analogue as inhibitors of microtubule polymerization and reverser of multidrug resistance

Xiaochao Huang; Rizhen Huang; Shaohua GouZhimei WangZhixin LiaoHengshan Wang

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Platinum(IV) complexes conjugated with phenstatin analogue as inhibitors of microtubule polymerization and reverser of multidrug resistance

机译：Platinum(IV) complexes conjugated with phenstatin analogue as inhibitors of microtubule polymerization and reverser of multidrug resistance

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Graphical abstract Display Omitted Highlights ? Complex 10 exhibited stronger antitumor activity and lower toxicity than cisplatin. ? Complex 10 effectively arrested NCI-H460 cells in G2/M stage. ? Tubulin polymerization assay indicated that 10 could inhibit tubulin polymerization in vitro . ? Representative complex 10 may induce apoptosis via two pathways. Abstract Pt(IV) complexes comprising a phenstatin analogue, as dual-targeting Pt(IV) prodrug, were designed and synthesized. They were found not only to carry the DNA binding platinum warhead into the tumor cells, but also to have a small molecular unit to inhibit tubulin polymerization. In vitro evaluation results revealed that Pt(IV) complexes showed better and more potent activity against the test human cancer cells including cisplatin resistant cell lines than their corresponding Pt(II) counterparts. In addition, the Pt(IV) derivative of cisplatin, complex 10 , exhibited highly selective inhibition in human cancer cells and displayed no obvious toxicity to two human normal cell lines, respectively. Mechanism study suggested that complex 10 induced cell-cycle arrest at the G2/M phase and caused apoptotic cell death of human lung cancer NCI-H460 cells through the mitochondrial mediated pathway. Moreover, complex 10 effectively inhibited the tumor growth in the NCI-H460 xenograft model. >

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《Bioorganic and medicinal chemistry》 |2017年第17期|4686-4700|共15页
作者
Xiaochao Huang; Rizhen Huang; Shaohua GouZhimei WangZhixin LiaoHengshan Wang;
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Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast;

State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Ministry;

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正文语种英语
中图分类药学;
关键词
Antitumor activity; Pt(IV) complex; Tubulin polymerization; Apoptosis;

Platinum(IV) complexes conjugated with phenstatin analogue as inhibitors of microtubule polymerization and reverser of multidrug resistance

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