研究动态
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芳基-烷基二有机锡芳基甲酰腙配合物的合成、抗癌活性和机理研究。

Synthesis, anticancer activity, and mechanistic investigations of aryl-alkyl diorganotin arylformylhydrazone complexes.

发表日期:2024 Oct 06
作者: Wujiu Jiang, Qing Luo, Wei Huang, Yuxing Tan, Yiyuan Peng
来源: JOURNAL OF INORGANIC BIOCHEMISTRY

摘要:

具有线粒体靶向作用的二有机锡酰腙复合物由于其有效的抗癌特性而显示出作为铂基复合物的替代品的巨大潜力。通过微波“一锅法”反应合成了12种甲基苯基锡芳基甲酰腙配合物。该配合物已通过 FT-IR、多核 NMR(1H、13C 和 119Sn)、TGA 和 HRMS 进行了表征。确定了所研究的 12 种配合物中 10 种的晶体结构。结构1至8、10和12具有双核Sn2O2四面体环的中心对称结构。测试了所有复合物对人类细胞系 NCI-H460、MCF-7 和 HepG2 的抑制活性。复合物8对HepG2细胞表现出最有效的抑制作用,IC50值为1.34±0.04μM。抗癌机制的初步研究表明,复合物8通过线粒体途径诱导HepG2细胞凋亡,并伴有G2/M期细胞周期阻滞。版权所有©2024。由Elsevier Inc.出版。
Diorganotin acylhydrazone complexes with mitochondrial targeting demonstrate significant potential as replacements for platinum-based complexes due to their potent anticancer properties. Twelve methylphenyltin arylformylhydrazone complexes have been synthesized by microwave "one-pot" reaction. The complexes have been characterized by FT-IR, multinuclear NMR (1H, 13C, and 119Sn), TGA, and HRMS. Crystal structures were determined for 10 out of the 12 complexes under study. Structures 1 through 8, 10 and 12 possessed a central symmetric structure of a di-nuclear Sn2O2 tetrahedral ring. All complexes were tested for their inhibitory activity against human cell lines NCI-H460, MCF-7, and HepG2. Complex 8 exhibited the most effective inhibitory effect on HepG2 cells, with an IC50 value of 1.34 ± 0.04 μM. Preliminary studies on the anticancer mechanism suggest that complex 8 induces apoptosis in HepG2 cells via the mitochondrial pathway, accompanied by G2/M phase cell cycle arrest.Copyright © 2024. Published by Elsevier Inc.