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

Bi-Qun ZouQi-Pin QinYu-Xia BaiQian-Qian CaoYe ZhangYan-Cheng LiuZhen-Feng ChenHong Liang
Published in: MedChemComm (2017)
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.
Keyphrases
  • dna damage
  • cell cycle arrest
  • oxidative stress
  • cell proliferation
  • single molecule
  • dna repair
  • drug delivery
  • signaling pathway
  • circulating tumor cells