Ruthenium(II) complexes containing PEGylated N-heterocyclic carbene ligands for tunning biocompatibility in the fight against cancer

IF 3.8 2区 化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Oscar Barrios , Claudia Inclán , Pablo Herrera , Alicia Bort , Avelino Martín , Jesús Cano , Inés Díaz-Laviada , Rafael Gómez
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Abstract

A synthetic procedure was designed for the preparation and characterization of Ag and Ru complexes containing NHC ligands functionalized with PEG fragments. Stability studies were conducted to gain insight of the species in water and other solvents like DMSO, or with reagents like imidazole as representative group for histidine amino acid. The presence of Cl atoms instead of H in the 4,5 positions of the N-heterocyclic carbene afforded higher water stability. The complexes containing PEG units must be considered inactive as anticancer agents. To enhance the anticancer activity of PEG-containing complexes, the balance between hydrophilicity and hydrophobicity was adjusted using a silane moiety, and an anionic carbosilane dendrimer as a lipophilic carrier.

Abstract Image

含有 PEG 化 N-heterocyclic carbene 配体的钌(II)配合物,用于调整抗癌过程中的生物相容性。
我们设计了一种合成程序,用于制备和表征含有 PEG 片段功能化 NHC 配体的 Ag 和 Ru 复合物。为了深入了解这些复合物在水和其他溶剂(如二甲基亚砜)或试剂(如作为组氨酸氨基酸代表基团的咪唑)中的稳定性,对它们进行了研究。N-heterocyclic carbene 的 4,5 位上存在 Cl 原子而不是 H 原子,因此在水中具有更高的稳定性。含有 PEG 单元的复合物必须被视为非活性抗癌剂。为了提高含 PEG 复合物的抗癌活性,我们使用硅烷分子和阴离子碳硅烷树枝状聚合物作为亲油载体来调节亲水性和疏水性之间的平衡。
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来源期刊
Journal of Inorganic Biochemistry
Journal of Inorganic Biochemistry 生物-生化与分子生物学
CiteScore
7.00
自引率
10.30%
发文量
336
审稿时长
41 days
期刊介绍: The Journal of Inorganic Biochemistry is an established international forum for research in all aspects of Biological Inorganic Chemistry. Original papers of a high scientific level are published in the form of Articles (full length papers), Short Communications, Focused Reviews and Bioinorganic Methods. Topics include: the chemistry, structure and function of metalloenzymes; the interaction of inorganic ions and molecules with proteins and nucleic acids; the synthesis and properties of coordination complexes of biological interest including both structural and functional model systems; the function of metal- containing systems in the regulation of gene expression; the role of metals in medicine; the application of spectroscopic methods to determine the structure of metallobiomolecules; the preparation and characterization of metal-based biomaterials; and related systems. The emphasis of the Journal is on the structure and mechanism of action of metallobiomolecules.
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