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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 ( IF 6.0 ) Pub Date : 2016-09-04 07:34:52
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

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.

中文翻译:

具有9,9-二己基-4,5-二氮芴的铂(II)和钯(II)配合物的合成及其对Hep3B异种移植小鼠的体内抗肿瘤活性

分别是二氯(9,9-二己基-4,5-二氮杂芴)铂(II)(Pt-DHF)和二氯(9,9-二己基-4,5-二氮杂芴)钯(II)(Pd-DHF)的配合物用异种移植了人类Hep3B癌细胞的无胸腺裸鼠模型研究了它们的合成,并研究了它们的体内抗肿瘤活性。与媒介物对照组相比,Pt-DHF和Pd-DHF治疗组显示出显着的肿瘤生长抑制作用(约9倍和3倍的肿瘤生长迟缓)。研究了这两种化合物对动物的肝脏毒理作用。Pt-DHF和Pd-DHF处理组的丙氨酸转氨酶和天冬氨酸转氨酶值均低于媒介物处理组,因为媒介物对照组的动物肝癌负担非常重。
更新日期:2016-09-04
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