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设计,合成和机械研究新型的arylformylhydrazone但ylphenyltin复合物作为潜在的抗癌剂

Wujiu Jiang¹, Shanji Fan², Zhihua Zhu³

¹Key Laboratory of Green Chemistry, Jiangxi Province, College of Chemistry and Chemical Engineering, Jiangxi Normal University, Nanchang, Jiangxi 330022, China; Key Laboratory of Functional Metal-Organic Compounds of Hunan Province, Key Laboratory of Organometallic New Materials, College of Hunan Province, College of Chemistry and Materials Science, Hengyang Normal University, Hengyang, Hunan 421008, China.

Bioorganic chemistry

|May 28, 2024

概括

新的不对称的dialkyltin复合物显示出强大的抗癌活性. 复合C2通过诱导亡和破坏线粒体功能,有效地抑制了HepG2细胞,突出了其治疗潜力.

科学领域:

有机金属化学有机金属化学
药用化学医学化学
癌症生物学癌症生物学

背景情况:

迪奥加诺丁复合物以其抗癌性质而闻名.
具有混合基团的不对称基化合物尚未得到充分的研究.
这项研究的重点是新型布基混合基丁基甲基甲基化复合物.

研究的目的:

为了合成和表征新的不对称的dialkyltin复合物.
为了评估这些复合物的体外抗癌活性,与各种人类细胞系对比.
为了阐明最强大的复合物的作用机制.

主要方法:

微波辅助的"一"合成20个丁基混合基丁基甲基甲基酸复合物.
使用X射线衍射测定九个复合物的晶体结构.
在实验室中对NCI-H460,MCF-7,HepG2,Huh-7和HL-7702细胞系进行细胞毒性测试.
细胞生物学试验包括诱导亡,细胞循环分析,线粒体膜潜能评估和反应性氧物种测量.
西部斑点分析以确认亡途径.

主要成果:

成功合成了二十种新型不对称的dialkyltin复合体.
晶体结构显示了双核Sn2O2或三核锡-氧气集群形成.
复合C2对HepG2细胞表现出显著的抑制作用 (IC50 = 0.82 ± 0.03μM).
在HepG2和Huh-7细胞中,复杂C2诱导的亡和G2/M细胞周期停止.
复杂的C2触发了线粒体功能障碍和反应性氧物种的增加.

结论:

不对称的二甲基丁甲基甲复合物代表了一类有前途的抗癌药物.
复合C2对肝细胞癌 (HepG2细胞) 具有强大和特异性的活性.
作用机制涉及线粒体通路介导的亡和氧化应激诱导.

关键词:

乙烯基化松是一种化.它具有抗癌活性.抗癌机制的抗癌机制但是基基的使用方法.有机蛋白是有机蛋白中的一种.综合合成综合合成

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Radical Substitution: Hydrogenolysis of Alkyl Halides with Tributyltin Hydride

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Radical substitution reactions can be used to remove functional groups from molecules. The hydrogenolysis of alkyl halides is one such reaction, where the weak Sn–H bond in tributyltin hydride reacts with alkyl halides to form alkanes. Here, the reagent Bu3SnH yields tributyltin halide as a byproduct.
The bonds formed in this reaction are stronger than the bonds broken, making it energetically favorable. The reaction follows a radical chain mechanism similar to radical halogenation...