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偕嗯啶酮腙配体钌（II）配合物的光细胞毒性活性。

Photocytotoxic Activity of Ruthenium(II) Complexes with Phenanthroline-Hydrazone Ligands.

机构信息

Departamento de Química, Centro Federal de Educação Tecnológica de Minas Gerais, Avenida Amazonas, 5253, Belo Horizontre (MG) 30421-169, Brazil.

Departamento de Química, Universidade Federal de Minas Gerais, Avenida Antônio Carlos, 6627, Belo Horizonte (MG) 31270-901, Brazil.

出版信息

Molecules. 2021 Apr 6;26(7):2084. doi: 10.3390/molecules26072084.

DOI:10.3390/molecules26072084
PMID:33917290
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8038675/
Abstract

This paper reports on the synthesis and characterization of two new polypyridyl-hydrazone Schiff bases, ()-'-(6-oxo-1,10-phenanthrolin-5(6)-ylidene)thiophene-2-carbohydrazide () and ()-'-(6-oxo-1,10-phenanthrolin-5(6)-ylidene)furan-2-carbohydrazide (), and their two Ru(II) complexes of the general formula RuCl(DMSO)(phen)(L). Considering that hydrazides are a structural part of severa l drugs and metal complexes containing phenanthroline derivatives are known to interact with DNA and to exhibit antitumor activity, more potent anticancer agents can be obtained by covalently linking the thiophene acid hydrazide or the furoic acid hydrazide to a 1,10-phenanthroline moiety. These ligands and the Ru(II) complexes were characterized by elemental analyses, electronic, vibrational, H NMR, and ESI-MS spectroscopies. Ru is bound to two different -heterocyclic ligands. One chloride and one S-bonded DMSO in -configuration to each other complete the octahedral coordination sphere around the metal ion. The ligands are very effective in inhibiting cellular growth in a chronic myelogenous leukemia cell line, K562. Both complexes are able to interact with DNA and present moderate cytotoxic activity, but 5 min of UV-light exposure increases cytotoxicity by three times.

摘要

本文报道了两种新的多吡啶-腙席夫碱的合成与表征，（）-（6-氧代-1,10-菲咯啉-5（6）-亚基）噻吩-2-甲酰腙（）和（）-（6-氧代-1,10-菲咯啉-5（6）-亚基）呋喃-2-甲酰腙（），以及它们的两个 Ru(II) 配合物，通式为 RuCl(DMSO)(phen)(L)。考虑到腙是几种药物的结构部分，并且已知含有菲咯啉衍生物的金属配合物与 DNA 相互作用并具有抗肿瘤活性，通过将噻吩酸腙或呋喃酸腙共价键合到 1,10-菲咯啉部分，可以获得更有效的抗癌剂。这些配体和 Ru(II) 配合物通过元素分析、电子、振动、H NMR 和 ESI-MS 光谱进行了表征。Ru 与两个不同的 -杂环配体键合。一个氯离子和一个 S 键合的 DMSO 以彼此相反的构型相互配合，完成了金属离子周围的八面体配位场。这些配体在慢性髓性白血病细胞系 K562 中非常有效地抑制细胞生长。两个配合物都能够与 DNA 相互作用并具有中等的细胞毒性活性，但 5 分钟的紫外线照射使细胞毒性增加了三倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/1acc9aff93d5/molecules-26-02084-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/b1352e0f0ae1/molecules-26-02084-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/d7d9a7523d13/molecules-26-02084-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/bf65e3394a5f/molecules-26-02084-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/8128e5f79299/molecules-26-02084-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/e23559a47b83/molecules-26-02084-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/1acc9aff93d5/molecules-26-02084-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/b1352e0f0ae1/molecules-26-02084-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/d7d9a7523d13/molecules-26-02084-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/bf65e3394a5f/molecules-26-02084-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/8128e5f79299/molecules-26-02084-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/e23559a47b83/molecules-26-02084-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7554/8038675/1acc9aff93d5/molecules-26-02084-g006.jpg

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