Synthesis and cytotoxicity study of water soluble 8-hydroxyquinoline stabilized zirconium(Ⅳ) complexes.

8-hydroxyquinoline coordinated zirconium(IV) complexes exhibit good aqueous solubility and stability, the cytotoxicity of them were significantly enhanced against human Hela S3, Hep G2 and PC9 cells than cisplatin but limited against normal AML12 cells. [Display omitted] • 8-hydroxyquinoline Zr(IV) complexes exhibit excellent aqueous stability and solubility. • One Zr(IV) complex showed significantly enhanced activity against Hep G2 cells than cisplatin. • These Zr(IV) complexes could almost exclusively induce the cell apoptosis of Hep G2 cells. Three octacoordinated zirconium(IV) tetrakis -(8-hydroxyquinolinate) complexes [(L 1-3) 4 Zr(IV)] were synthesized smoothly in THF at room temperature using ZrCl 4 as a starting material with yields ranging from 74% to 83%. Their structures were characterized by 1H, 13C NMR and X-ray diffraction spectroscopy. [(L 1-3) 4 Zr(IV)] exhibited excellent solubility and stability in H 2 O and DMSO, and they have demonstrated enhanced cytotoxicity against human Hep G2, Hela S3 and PC9 cells than cisplatin. Among them, [(L 1) 4 Zr(IV)] bearing non-substituted 8-hydroxyquinoline showed about 2 orders of magnitude higher inhibition activity against Hep G2 cells than cisplatin (IC 50 : 0.14 ± 0.1 μM, cisplatin: 13.82 ± 1.3 μM). The selectivity towards tumor cells was preliminary evidenced by their partial or completely vanished inhibition activity against AML12 cells. Additionally, [(L 1) 4 Zr(IV)] could almost exclusively induce the apoptosis of Hep G2 cells. [ABSTRACT FROM AUTHOR]