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基于硫代吡唑的新型'-钯(铂)配合物的合成及其抗癌活性研究。

Synthesis of new ,'-Pd(Pt) complexes based on sulfanyl pyrazoles, and investigation of their anticancer activity.

作者信息

Akhmetova Vnira R, Akhmadiev Nail S, Abdullin Marat F, Dzhemileva Lilya U, D'yakonov Vladimir A

机构信息

Institute of Petrochemistry and Catalysis, Russian Academy of Sciences 141 Prospekt Oktyabrya 450075 Ufa Russian Federation

Ufa Institute of Chemistry, Russian Academy of Sciences 71 Prospekt Oktyabrya 450054 Ufa Russian Federation.

出版信息

RSC Adv. 2020 Apr 17;10(26):15116-15123. doi: 10.1039/c9ra09783j. eCollection 2020 Apr 16.

Abstract

The synthesis of new ,'-mononuclear bi-ligand Pd(ii) and tri-ligand Pt(ii)complexes bearing sulfanyl(phenyl, benzyl, cyclohexyl, 4-hydroxyphenyl)3,5-dimethyl-1-pyrazole ligands has been carried out. The obtained compounds were studied for apoptosis-inducing activity and effect on the cell cycle for Jurkat, K562, and U937 neoplastic cell cultures and conditionally normal human embryonic kidney HEK293 cells. The cells showed the highest sensitivity to platinum and palladium complexes in comparison with ligands and cisplatin. The cytotoxic properties are enhanced for compounds with cyclohexyl substituents at the S-atom in sulfanyl pyrazoles and complexes.

摘要

已合成了带有硫烷基(苯基、苄基、环己基、4-羟基苯基)3,5-二甲基-1-吡唑配体的新型单核双配体钯(II)和三配体铂(II)配合物。对所获得的化合物进行了研究,考察其对Jurkat、K562和U937肿瘤细胞培养物以及条件性正常人类胚胎肾HEK293细胞的凋亡诱导活性和对细胞周期的影响。与配体和顺铂相比,细胞对铂和钯配合物表现出最高的敏感性。对于硫烷基吡唑和配合物中S原子带有环己基取代基的化合物,其细胞毒性特性增强。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7830/9052211/97acae7eef01/c9ra09783j-f1.jpg

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