Synthesis of platinum(II) and palladium(II) complexes with 9,9-dihexyl-4,5-diazafluorene and their in vivo antitumour activity against Hep3B xenografted mice.

Abstract

Two complexes dichloro(9,9-dihexyl-4,5-diazafluorene)platinum(II) (Pt-DHF) and dichloro(9,9-dihexyl-4,5-diazafluorene)palladium(II) (Pd-DHF) were synthesized and their in vivo antitumour activity was investigated using an athymic nude mice model xenografted with human Hep3B carcinoma cells. Pt-DHF- and Pd-DHF-treated groups showed significant tumour growth inhibition (with about 9-fold and 3-fold tumour growth retardation) when compared with the vehicle control group. The liver toxicology effects on the animals of the two compounds were investigated. Pt-DHF and Pd-DHF-treated groups had a lower alanine transaminase and aspartate transaminase values than those of the vehicle treated group as the animals from the vehicle control group had very heavy hepatoma burden. We assume that both complexes could be further investigated as effective antitumour agents and it is worthwhile to study their underlying working mechanism.

• Authors: Q-W Wang, P-L Lam, R S-M Wong, G Y-M Cheng, K-H Lam, Z-X Bian, C-L Ho, Y-H Feng, R Gambari, Y-H Lo, W-Y Wong, C-H Chui
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 124 Pg. 537-543 (Nov 29 2016) ISSN: 1768-3254 [Electronic] France
• PMID: 27598239 (Publication Type: Journal Article)
• Copyright: Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antineoplastic Agents
• Coordination Complexes
• Organoplatinum Compounds
• dichloro(9,9-dihexyl-4,5-diazafluorene)palladium(II)
• dichloro(9,9-dihexyl-4,5-diazafluorene)platinum(II)
• Platinum
• Palladium

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology, therapeutic use)
• Carcinoma, Hepatocellular (drug therapy)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Coordination Complexes (chemical synthesis, chemistry, pharmacology)
• Disease Models, Animal
• Enzyme Activation (drug effects)
• Heterografts
• Humans
• Liver (drug effects)
• Liver Neoplasms (drug therapy)
• Mice
• Organoplatinum Compounds (chemical synthesis, chemistry, pharmacology, therapeutic use)
• Palladium (chemistry, pharmacology, therapeutic use)
• Platinum (chemistry, pharmacology, therapeutic use)