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的合成和表征 (II) 氨酸环素复合物与氨酸衍生物作为抗癌剂

Brondwyn S McGhie¹, Jennette Sakoff², Jayne Gilbert²

¹Nanoscale Organisation and Dynamics Group, School of Science, Western Sydney University, Locked Bag 1797, Penrith, NSW 2751, Australia.

International journal of molecular sciences

|December 23, 2023

概括

新型 (II) 复合物显示出有前途的抗癌活性,为传统化疗提供了替代品,副作用减少,对特定癌症细胞系的疗效提高.

科学领域:

药用化学医学化学
在瘤学瘤学.
有机金属化学有机金属化学

背景情况:

西斯普拉丁类型的化疗药物在癌症治疗中至关重要,但面临副作用和耐药性的挑战.
研究主要集中在西斯和其衍生品上,使得新复合体设计的潜力未被探索.

研究的目的:

合成和表征新的有机金属 (II) 复合物,其灵感来源于与其他金属使用的设计.
评估这些新复杂物作为抗癌剂的DNA结合亲和性,脂性和细胞毒性潜力.

主要方法:

六种新型Pt(II) 复合物的合成和表征,这些复合物具有不同的P_L连接物 (2-pyrrolidin-2-ylpyridine,2-{1H-Imidazol-2-yl) pyridine,2-{2-pyridyl) benzimidazole) 和一个常见的A_L连接物 (diaminocyclohexane).
对各种癌症细胞系的DNA结合相互作用和细胞毒性的评估.
新型复合物与前体化合物和已确定的复合物 (如56MESS) 的比较.

主要成果:

新型的[Pt(P_L) L) ]²⁺复合体显示出有前途的细胞毒性,与西斯普拉丁相当或优于它.
与西斯相比,这些复合物表现出明显的DNA结合相互作用.
与2-pyrrolidin-2-ylpyridine和2-(2-pyridyl) benzimidazole连接体的复合体在MCF10A和MCF-7乳腺癌细胞系中显示出显著的选择性指数.

结论:

合成的有机金属Pt(II) 复合物代表了一种有前途的新型抗癌药物.
这些新型复合物比传统的制药具有潜在的优势,包括改变DNA结合和提高选择性.
对这些复合物的进一步研究可能会导致开发更有效,更有针对性的癌症疗法.

关键词:

抗癌药物抗癌药物抗癌药物伊米达尔 (Imidazole) 是一种金复合体中的金复合体.皮里丁的衍生品是皮里丁的衍生品.

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Stereoisomerism

Stereoisomerism

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...