铜的合成,结构和稳定性 (II) 含有具有潜在抗癌活性的伊米达佐林-他联体的复合体
Łukasz Balewski1, Iwona Inkielewicz-Stępniak2, Maria Gdaniec3
1Department of Chemical Technology of Drugs, Faculty of Pharmacy, Medical University of Gdansk, Gen. J. Hallera 107, 80-416 Gdańsk, Poland.
Pharmaceuticals (Basel, Switzerland)
|March 27, 2025
概括
这项研究合成了铜 (II) 复合物作为潜在的抗癌剂. 复合C2对三阴性乳腺癌细胞表现出显著的抗瘤活性,没有观察到抗菌作用.
科学领域:
- 药用化学 医学化学
- 无机化学 无机化学
- 癌症研究 癌症研究
背景情况:
- 越来越多的人对金属制药作为新型抗癌剂的兴趣.
- 铜 (II) 复合物的勘探,这些复合物是从fthalazine和imidazoline连接物中衍生出来的.
- 评估生物活动,包括抗癌,抗微生物和抗氧化物质.
研究的目的:
- 合成和表征两种铜 (C1和C2) 复合物,其中含有基于甲和依米达的配体.
- 评估这些复合体对人类癌细胞系 (HeLa,MCF-7,MDA-MB-231) 和非瘤细胞系 (HDFa) 的体外细胞毒性作用.
- 评估合成化合物的抗菌和抗氧化潜力.
主要方法:
- 通过元素分析,红外光谱学和X射线衍射,合成和描述连接物 (L1-L3) 和铜 (II) 复合物 (C1-C2).
- 通过MTT测定进行细胞毒性评估.
- 对黄金葡萄球菌,大肠杆菌和白菌的抗菌活性测试.
- 使用ABTS,DPPH和FRAP测定进行抗氧化活性评估.
- 在 silico ADME 预测药物相似性.
主要成果:
- 铜 (II) 复合物C2对MDA-MB-231细胞表现出显著的抗瘤活性,与西斯普拉丁相当.
- 与西斯普拉丁相比,C1和C2复合体对正常的HDFa细胞的细胞毒性较低.
- 化合物对HeLa,MCF-7和MDA-MB-231细胞表现出适度的抗癌作用 (57.5-81.2%的活力降低为C2).
- 没有观察到任何测试化合物的显著抗菌或抗真菌活性.
- 在ABTS测定中,联体L1显示了中度的抗激素活性 (IC50=23.63μg/mL).
结论:
- 铜 (II) 复合体C2,具有fthalazin-1 (H) -one支架,是一种强大的抗癌剂候选物.
- 对潜在的治疗应用来说,缺乏抗菌活性是有利的.
- 连接物L1具有中度的抗氧化特性,有助于整体生物特征.
相关概念视频
02:57Coordination Number and Geometry
15.4K
For transition metal complexes, the coordination number determines the geometry around the central metal ion. Table 1 compares coordination numbers to molecular geometry. The most common structures of the complexes in coordination compounds are octahedral, tetrahedral, and square planar.
15.4K
02:52Stereoisomerism
11.7K
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...
11.7K
02:51Metal-Ligand Bonds
20.4K
The hemoglobin in the blood, the chlorophyll in green plants, vitamin B-12, and the catalyst used in the manufacture of polyethylene all contain coordination compounds. Ions of the metals, especially the transition metals, are likely to form complexes.
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
20.4K
03:02Colors and Magnetism
11.4K
Color in Coordination Complexes
When atoms or molecules absorb light at the proper frequency, their electrons are excited to higher-energy orbitals. For many main group atoms and molecules, the absorbed photons are in the ultraviolet range of the electromagnetic spectrum, which cannot be detected by the human eye. For coordination compounds, the energy difference between the d orbitals often allows photons in the visible range to be absorbed and emitted, which is seen as colors by the human...
When atoms or molecules absorb light at the proper frequency, their electrons are excited to higher-energy orbitals. For many main group atoms and molecules, the absorbed photons are in the ultraviolet range of the electromagnetic spectrum, which cannot be detected by the human eye. For coordination compounds, the energy difference between the d orbitals often allows photons in the visible range to be absorbed and emitted, which is seen as colors by the human...
11.4K
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,...
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,...
19.1K