研究动态
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带有取代的 2-(1H-苯并咪唑-2-基)喹啉的新型环金属化铱 (III) 配合物:合成、表征、电化学和抗癌研究。

New cyclometalated iridium(III) complexes bearing substituted 2-(1H-benzimidazol-2-yl)quinoline: Synthesis, characterization, electrochemical and anticancer studies.

发表日期:2024 Aug 08
作者: Cigdem Sahin, Dogukan Mutlu, Ahmet Erdem, Rafet Kilincarslan, Sevki Arslan
来源: BIOORGANIC CHEMISTRY

摘要:

带有不同侧基(苄基、2,3,4,5,6-五甲基苄基和 2,3,4, 5,6-五氟苄基)的合成和表征通过光谱分析。研究了铱化合物不同侧基对光物理和电化学性能的影响。已使用多种方法(包括 MTT 测定、流式细胞术、qRT-PCR 和集落形成)评估了这些化合物对乳腺癌细胞系的细胞毒性和细胞凋亡。 C1 的细胞毒性(以 IC50 值表示)对于 MDA-MB-231 为 11.76 μM,对于 MCF-7 细胞为 5.35 μM。对于 C3,MDA-MB-231 的 IC50 值为 16.22 μM,MCF-7 细胞的 IC50 值为 8.85 μM。在这两种细胞系中,均观察到 Bax 和 caspase 3 水平升高,以及 BCL-2 下调和膜联蛋白 V 染色阳性,证实了细胞凋亡。此外,C1 和 C3 复合物处理后,两种细胞系的集落形成能力均下降。所有这些结果表明,化合物 C1 和 C3 可能具有治疗乳腺癌的潜力,但还需要进一步研究来证实其功效。版权所有 © 2024 Elsevier Inc. 保留所有权利。
New iridium(III) compounds (C1-C3) bearing 2-(1H-benzimidazol-2-yl)quinoline ligands with different side groups (benzyl, 2,3,4,5,6-pentamethylbenzyl and 2,3,4,5,6-pentafluorobenzyl) were synthesized and characterized by using spectroscopic analyses. The effects of different side groups of iridium compounds on the photophysical and electrochemical properties have been investigated. The cytotoxicity and apoptosis of the compounds have been evaluated on breast cancer cell lines using various methods including MTT assay, flow cytometry, qRT-PCR, and colony formation. The cytotoxicity of C1, expressed as IC50 values, was found to be 11.76 μM for MDA-MB-231 and 5.35 μM for MCF-7 cells. For C3, the IC50 value was 16.22 μM for MDA-MB-231 and 8.85 μM for MCF-7 cells. In both cell lines, increased levels of Bax and caspase 3, along with downregulation of BCL-2 and positive annexin V staining, were observed, confirming apoptosis. Moreover, the colony-forming abilities in both cell lines decreased after C1 and C3 complex treatment. All these results suggest that the compounds C1 and C3 may have potential in the treatment of breast cancer, though further research is needed to confirm their efficacy.Copyright © 2024 Elsevier Inc. All rights reserved.