从2,6-diacetylpyridine bis(2-hydroxybenzoylhydrazone) 衍生的有机 (IV) 复合物作为潜在的抗增殖剂:合成,表征,结构和体外抗癌活性
Tushar S Basu Baul1, Bietlaichhai Hlychho2, Siddhartha Das Pramanik3
1Centre for Advanced Studies in Chemistry, North-Eastern Hill University, NEHU Permanent Campus, Umshing, Shillong 793 022, India; Sophisticated Analytical Instrument Facility, North-Eastern Hill University, NEHU Permanent Campus, Umshing, Shillong 793 022, India.
Journal of inorganic biochemistry
|August 29, 2024
概括
新的有机素 (IV) 复合物显示出对前列腺癌细胞有强大的抗增殖作用. 迪布提林化合物2显示出显著的活性,通过活性氧物种生成诱导亡,为化疗提供了一个有前途的替代方案.
科学领域:
- 有机金属化学 有机金属化学
- 药用化学 医学化学
- 癌症研究 癌症研究
背景情况:
- 机体蛋白 (IV) 复合体因其多样化的生物活动而被探索.
- 开发新的抗癌药物对于有效治疗前列腺癌至关重要.
- 连接体 2,6-diacetylpyridine bis(2-hydroxybenzoylhydrazone) (H2L) 为协调化学提供了一个多功能支架.
研究的目的:
- 为了合成和表征新的有机 (IV) 复合物.
- 评估这些复杂物对前列腺癌细胞的抗增殖活性.
- 为了研究最活跃的化合物的作用机制.
主要方法:
- 使用FT-IR,HRMS,FT-NMR和SC-XRD合成和表征六种有机素 (IV) 复合物.
- 对DU-145前列腺癌细胞和HEK-293正常细胞的抗增殖活性的评估.
- 使用AO/EB染色和ROS生成试验的作用研究的机制.
主要成果:
- 六种新的七协调单核有机蛋白 (IV) 复合物已成功合成并从结构上阐明.
- 迪布提林化合物2对DU-145细胞表现出显著的抗增殖活性 (IC50 = 6.16 ± 1.56 μM).
- 化合物2通过形态变化和活性氧物种生成诱导了亡.
结论:
- 合成的有机 (IV) 复合物,特别是二乙化合物2,显示出有前途的抗癌潜力.
- 抗增殖效应由亡诱导介导,涉及ROS生成.
- 这些化合物代表了传统化疗剂的潜在替代品.
相关概念视频
01:26Radical Substitution: Hydrogenolysis of Alkyl Halides with Tributyltin Hydride
1.8K
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...
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...
1.8K
02:52Stereoisomerism
11.8K
Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
11.8K
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