High antitumor activity of 5,7-dihalo-8-quinolinolato cerium complexes
摘要:
Three cerium complexes: [Ce(ClQ)(4)] (1) (H-ClQ = 5,7-dichloro-8-hydroxylquinoline), [Ce(ClIQ)(4)]center dot CH2Cl2 center dot 0.5H(2)O (2) (H-ClIQ = 5-chloro-7-iodo-8-hydroxylquinoline) and [Ce-2(BrQ)(4)(H-BrQ)(H2O)(3)Cl-2]center dot 1.5H(2)O (3) (H-BrQ = 5,7-dibromo-8-hydroxylquinoline) were synthesized. The structures of 1 and 2 are mononuclear whereas 3 has a binuclear structure. Compared with the H-ClQ H-CIIQ and H-BrQ complexes 1-3 exhibited significantly higher cytotoxicity (IC50 = 0.09-5.23 mu M) to SK-OV-3 and BEL-7404, 1 and 2 exhibited higher cytotoxicity to NCI-H460. Most the complexes and ligands exhibited higher cytotoxicity than cisplatin. Complexes 1-3 are much more sensitive to SK-OV-3 than to human normal liver cell HL-7702. Their antitumor activities were achieved through cell apoptosis and arrest at G0/G1-phase. Studies on the binding properties of 1-3 to DNA indicate that intercalation is the most probable binding mode. (C) 2013 Elsevier Masson SAS. All rights reserved.
Three cerium complexes: [Ce(ClQ)(4)] (1) (H-ClQ = 5,7-dichloro-8-hydroxylquinoline), [Ce(ClIQ)(4)]center dot CH2Cl2 center dot 0.5H(2)O (2) (H-ClIQ = 5-chloro-7-iodo-8-hydroxylquinoline) and [Ce-2(BrQ)(4)(H-BrQ)(H2O)(3)Cl-2]center dot 1.5H(2)O (3) (H-BrQ = 5,7-dibromo-8-hydroxylquinoline) were synthesized. The structures of 1 and 2 are mononuclear whereas 3 has a binuclear structure. Compared with the H-ClQ H-CIIQ and H-BrQ complexes 1-3 exhibited significantly higher cytotoxicity (IC50 = 0.09-5.23 mu M) to SK-OV-3 and BEL-7404, 1 and 2 exhibited higher cytotoxicity to NCI-H460. Most the complexes and ligands exhibited higher cytotoxicity than cisplatin. Complexes 1-3 are much more sensitive to SK-OV-3 than to human normal liver cell HL-7702. Their antitumor activities were achieved through cell apoptosis and arrest at G0/G1-phase. Studies on the binding properties of 1-3 to DNA indicate that intercalation is the most probable binding mode. (C) 2013 Elsevier Masson SAS. All rights reserved.