Department of Chemistry; School of Chinese Medicine
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.
Platinum-diazafluorene complex, Palladium-diazafluorene complex, Antitumour, In vivo
Source Publication Title
European Journal of Medicinal Chemistry
© 2016 Elsevier Masson SAS. All rights reserved.
This work is supported by the Innovation and Technology Commission to ABCT, HKPU, and the account codes: FRG1/14–15/021, FRG1/14–15/078 and 38-40-116 (C. H. Chui) as well as 03-16-176 (X. Z. Bian). R. Gambari is supported by AIRC (IG-13575). We thank the National Natural Science Foundation of China (project number: 51373145), Hong Kong Research Grants Council (HKBU12304715), Areas of Excellence Scheme of HKSAR (AoE/P-03/08), the Science, Technology and Innovation Committee of Shenzhen Municipality (JCYJ20140419130507116 and JCYJ20140818163041143) and Hong Kong Baptist University (FRG1/14-15/084) for financial support. The work was also supported by Partner State Key Laboratory of Environmental and Biological Analysis (SKLP-14-15-P011) and Strategic Development Fund of HKBU. Q. Wang and C.-L. Ho thank the International Science and Technology Cooperation Program of Chengdu (2014-GH02-00014-HZ) for financial support. Y. H. Lo gratefully acknowledges the financial support from the National Science Council of Taiwan (NSC 102-2113-M-845-001) and the project of the specific research fields in the University of Taipei, Taiwan.
Link to Publisher's Edition
Wang, Q., Lam, P., Wong, R., Cheng, G., Lam, K., Bian, Z., Ho, C., Feng, Y., Gambari, R., Lo, Y., Wong, W., & Chui, C. (2016). 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. European Journal of Medicinal Chemistry, 124, 537-543. https://doi.org/10.1016/j.ejmech.2016.08.033