相关实验视频
Updated: Jun 12, 2025
06:40
Synthesis of a Water-soluble Metal–Organic Complex Array
Published on: October 8, 2016
9.8K
探索新型NH形式的基基 schiff 基及其金属复合物:合成,表征,细胞毒性活性,分子对接和ADME研究
Elham S Aazam1, Maryam Majrashi1, Mostafa A Hussien1,2
1Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah, 21589, B.O. Box 80203, Saudi Arabia.
Heliyon
|September 23, 2024
概括
这项研究表明,基于树脂醇的希夫基础金属复合物对乳腺癌细胞具有显著的细胞毒性. 铜 (II) 和 (II) 复合物是最有效的,其性能优于标准药物5-Fluorouracil.
科学领域:
- 材料化学 材料化学
- 药用化学 医学化学
- 生物化学 生物化学
背景情况:
- 希夫基和它们的金属复合物被用于治疗应用.
- 基于Resorcinol的Schiff基提供了独特的结构性质,用于复杂化.
- 乳腺癌仍然是一个重大的全球健康挑战,需要新的治疗药物.
研究的目的:
- 为了合成和表征一种基于树脂素的希夫基 (HL) 和其Zn,Cd,Cu,Ni和Ni的复合物.
- 评估这些化合物对人类乳腺癌细胞MCF-7的体外细胞毒性作用.
- 研究这些复合物作为抗癌剂的潜力,包括与标准药物进行比较和分子对接研究.
主要方法:
- 通过质谱学,元素分析,UV-Vis,IR,ESR和X射线晶体学进行合成和结构性表征.
- 用MTT测定对MCF-7细胞进行细胞毒性评估,以确定IC50值.
- 对抗芳酶细胞染色体P450 (PDB: 3eqm) 和ADME预测的分子对接模拟.
主要成果:
- 希夫基联体 (HL) 呈现出一种混合型化物-化物结构.
- 所有合成的金属复合物都显示出对MCF-7细胞的显著细胞毒性 (IC50<38.37μM).
- (II) 和 (II) 复合物表现出优异的活性,超过自由配体和抗癌药物5-Fluorouracil (5-FU) 的13倍以上.
- 分子对接表明与目标芳酶细胞染色体P450.0的良好相互作用.
结论:
- 基于Resorcinol的希夫基础金属复合物对乳腺癌细胞具有强烈的细胞毒性活性.
- (II) 和 (II) 复合物代表了作为抗癌疗法进一步开发的有希望的候选人.
- 这项研究为设计针对乳腺癌途径的新型金属基抗癌药物提供了基础.
相关概念视频
01:26Synthesis of α-Substituted Carbonyl Compounds: The Stork Enamine Reaction
3.3K
α-Substituted ketones or aldehydes can be synthesized from enamines by the Stork enamine reaction, named after its pioneer Gilbert Stork. Enamines are useful synthetic intermediates where the lone pair on nitrogen is in conjugation with the C=C bond. They resemble enolate ions, as the resonance forms of both species have a nucleophilic α carbon.
3.3K
01:19Diazonium Group Substitution: –OH and –H
2.7K
Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
2.7K
02:34Structural Isomerism
19.1K
Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula. Structural isomerism of coordination compounds can be divided into two subcategories, the linkage isomers and coordination-sphere isomers.
Linkage isomers occur when the coordination compound contains a ligand that can bind to the transition metal center through two different atoms. For example, the CN− ligand can bind through the carbon atom or through the nitrogen atom. Similarly, SCN− can...
Isomers are different chemical species that have the same chemical formula. Structural isomerism of coordination compounds can be divided into two subcategories, the linkage isomers and coordination-sphere isomers.
Linkage isomers occur when the coordination compound contains a ligand that can bind to the transition metal center through two different atoms. For example, the CN− ligand can bind through the carbon atom or through the nitrogen atom. Similarly, SCN− can...
19.1K
01:30Nucleophilic Aromatic Substitution: Addition–Elimination (SNAr)
3.8K
Nucleophilic substitution in aromatic compounds is feasible in substrates bearing strong electron-withdrawing substituents positioned ortho or para to the leaving group. The reaction proceeds via two steps: the addition of the nucleophile and the elimination of the leaving group.
The reaction begins with an attack of the nucleophile on the carbon that holds the leaving group. This results in the delocalization of the π electrons over the ring carbons. The resonance interaction between...
The reaction begins with an attack of the nucleophile on the carbon that holds the leaving group. This results in the delocalization of the π electrons over the ring carbons. The resonance interaction between...
3.8K
01:16Aldehydes and Ketones with Amines: Imine and Enamine Formation Overview
4.5K
Primary amines react with carbonyl compounds—aldehydes and ketones—to generate imines. Imines consist of a C=N double bond and are named Schiff bases after its discoverer—the German chemist Hugo Schiff. On the other hand, secondary amines react with carbonyl compounds to give enamines. In enamines, the presence of a C=C double bond adjacent to the nitrogen atom leads to the delocalization of the lone pair.
4.5K
01:14Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
2.1K
Treating arylamines with nitrous acid gives aryldiazonium salts that are effective substrates in nucleophilic aromatic substitution reactions. The diazonio group in these salts can be easily displaced by different nucleophiles, yielding a wide variety of substituted benzenes. The leaving group departs as nitrogen gas, and this easy elimination is the driving force for the substitution reaction.
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
2.1K