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Synthesis and antitumor mechanism of a new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol as ligands.


ABSTRACT: 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 ?M. 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.

SUBMITTER: Zou BQ 

PROVIDER: S-EPMC6072324 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Synthesis and antitumor mechanism of a new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol as ligands.

Zou Bi-Qun BQ   Qin Qi-Pin QP   Bai Yu-Xia YX   Cao Qian-Qian QQ   Zhang Ye Y   Liu Yan-Cheng YC   Chen Zhen-Feng ZF   Liang Hong H  

MedChemComm 20170201 3


A new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, <i>i.e.</i>, [Fe(ClMQ)<sub>2</sub>Cl] (<b>1</b>), was synthesized and evaluated for its anticancer activity. Compared to the HClMQ ligand, complex <b>1</b> showed a higher cytotoxicity towards a series of tumor cell lines, including Hep-G2, BEL-7404, NCI-H460, A549, and T-24, with IC<sub>50</sub> values in the range of 5.04-14.35 μM. Notably, the Hep-G2 cell line was the most sensitive to complex <b>1</b>. Mechan  ...[more]

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