Planar Chiral Ferrocene Cyclopalladated Derivatives Induce Caspase-Dependent Apoptosis and Antimetastasis in Cancer Cells

Planar Chiral Ferrocene Cyclopalladated Derivatives Induce Caspase-Dependent Apoptosis and Antimetastasis in Cancer Cells
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平面手性二茂铁环钯化衍生物诱导癌细胞中半胱天冬酶依赖性细胞凋亡和抗转移

DOI:
10.1021/acs.organomet.7b00897
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发表时间:
2018-03
期刊:
影响因子:
2.8
通讯作者:
Zhao Gang
Zhao Gang
中科院分区:
化学2区
文献类型:
--
作者:
Gong Guidong;Cao Yuan;Wang Fei;Zhao Gang

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合成并表征了一系列平面手性二茂铁环钯化合物。通过单晶X-射线衍射分析确定了四个化合物的绝对构型。合成的化合物和顺铂的细胞毒活性对人肝癌、乳腺癌和结肠癌细胞系的活力表现出不同的抑制效力。双核化合物7在肝癌细胞中的作用是顺铂的16倍。化合物7在抑制肝癌细胞转移方面也比顺铂更有效。流式细胞仪分析和半胱天冬酶活性测定表明,化合物7通过诱导半胱天冬酶依赖性凋亡在癌细胞中发挥抗增殖活性。
A series of planar chiral ferrocene cyclopalladated compounds were synthesized and characterized. The absolute configurations of four compounds were determined by single-crystal X-ray analysis. The cytotoxic activities of the synthesized compounds and cisplatin exhibited different inhibition potencies on the viability of human liver, breast, and colon cancer cell lines. The dinuclear compound 7 was 16-fold more potent than cisplatin in hepatoma cells. Compound 7 was also more effective than cisplatin in the inhibition of hepatoma cell metastasis. Flow cytometry analysis and caspase activity assays indicated that compound 7 exerted antiproliferative activity in cancer cells through the induction of caspase-dependent apoptosis.
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