Synthesis and antitumor mechanism of a new ironIJIII) complex with 5,7-dichloro-2-methyl-8quinolinol as ligands
Synthesis and antitumor mechanism of a new ironIJIII) complex with 5,7-dichloro-2-methyl-8quinolinol as ligands
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以5,7-二氯-2-甲基-8喹啉醇为配体的新型铁(III)配合物的合成及抗肿瘤机制
DOI：
10.1039/c6md00644b
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发表时间：
2017
期刊：
影响因子：
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通讯作者：
Hong Liang
中科院分区：
文献类型：
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作者：
Bi-Qun Zou;Qi-Pin Qin;Yu-Xia Bai;Qian-Qian Cao;Ye Zhang;Yan-Cheng Liu;Zhen-Feng Chen;Hong Liang
以5，7-二氯-2-甲基-8-羟基喹啉（HClMQ）为配体的新铁（III）配合物，[Fe（ClMQ）2Cl]（1）的合成及其抗癌活性。与HClMQ配体相比，配合物1对一系列肿瘤细胞系（包括Hep-G2、BEL-7404、NCI-H460、A549和T-24）显示出更高的细胞毒性，IC 50值在5.04-14.35 μM范围内。值得注意的是，Hep-G2细胞系对复合物1最敏感。机制研究表明，复合物1是一种靶向c-myc G-四链体DNA的端粒酶抑制剂，可通过诱导细胞周期阻滞和DNA损伤而引发细胞凋亡。
A new iron(III) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, i.e., [Fe(ClMQ)2Cl] (1), was synthesized and evaluated for its anticancer activity. Compared to the HClMQ ligand, complex 1 showed a higher cytotoxicity towards a series of tumor cell lines, including Hep-G2, BEL-7404, NCI-H460, A549, and T-24, with IC50 values in the range of 5.04–14.35 μM. Notably, the Hep-G2 cell line was the most sensitive to complex 1. Mechanistic studies indicated that complex 1 is a telomerase inhibitor targeting c-myc G-quadruplex DNA and can trigger cell apoptosis via inducing cell cycle arrest and DNA damage.