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

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

doi:10.1016/j.ejmech.2016.08.033

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

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^*

^*Corresponding author for this work

Research output: Contribution to journal › Journal article › peer-review

11 Citations (Scopus)

70 Downloads (Pure)

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.

Original language	English
Pages (from-to)	537-543
Number of pages	7
Journal	European Journal of Medicinal Chemistry
Volume	124
Early online date	18 Aug 2016
DOIs	https://doi.org/10.1016/j.ejmech.2016.08.033
Publication status	Published - Nov 2016

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

User-Defined Keywords

Platinum-diazafluorene complex
Palladium-diazafluorene complex
Antitumour
In vivo

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10.1016/j.ejmech.2016.08.033

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Wang, Q.-W., Lam, P.-L., Wong, R. S.-M., Cheng, G. Y.-M., Lam, K.-H., Bian, Z.-X., Ho, C.-L., Feng, Y.-H., Gambari, R., Lo, Y.-H., Wong, W.-Y., & Chui, C.-H. (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

@article{8f94f5bef0994bd481394158df596486,

title = "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.",

keywords = "Platinum-diazafluorene complex, Palladium-diazafluorene complex, Antitumour, In vivo",

author = "Q.-W. Wang and P.-L. Lam and Wong, \{R. S.-M.\} and Cheng, \{G. Y.-M.\} and K.-H. Lam and Z.-X. Bian and C.-L. Ho and Y.-H. Feng and R. Gambari and Y.-H. Lo and W.-Y. Wong and C.-H. Chui",

note = "Funding Information: 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. ",

year = "2016",

month = nov,

doi = "10.1016/j.ejmech.2016.08.033",

language = "English",

volume = "124",

pages = "537--543",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

Wang, Q-W, Lam, P-L, Wong, RS-M, Cheng, GY-M, Lam, K-H, Bian, Z-X, Ho, C-L, Feng, Y-H, Gambari, R, Lo, Y-H, Wong, W-Y & Chui, C-H 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, vol. 124, pp. 537-543. https://doi.org/10.1016/j.ejmech.2016.08.033

TY - JOUR

T1 - 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

AU - Wang, Q.-W.

AU - Lam, P.-L.

AU - Wong, R. S.-M.

AU - Cheng, G. Y.-M.

AU - Lam, K.-H.

AU - Bian, Z.-X.

AU - Ho, C.-L.

AU - Feng, Y.-H.

AU - Gambari, R.

AU - Lo, Y.-H.

AU - Wong, W.-Y.

AU - Chui, C.-H.

N1 - Funding Information: 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.

PY - 2016/11

Y1 - 2016/11

N2 - 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.

AB - 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.

KW - Platinum-diazafluorene complex

KW - Palladium-diazafluorene complex

KW - Antitumour

KW - In vivo

UR - https://www.scopus.com/pages/publications/84985930755

U2 - 10.1016/j.ejmech.2016.08.033

DO - 10.1016/j.ejmech.2016.08.033

M3 - Journal article

C2 - 27598239

AN - SCOPUS:84985930755

SN - 0223-5234

VL - 124

SP - 537

EP - 543

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -