Design, Synthesis, Characterization, and Antitumor Activities of Benzimidazole-functionalized Organoruthenium Complexes Bearing Fluorine Group.

IF 1.9 4区医学 Q3 CHEMISTRY, MEDICINAL

Medicinal Chemistry Pub Date : 2025-02-11 DOI:10.2174/0115734064331622241113032042

Ramazan Paşahan, Özlem Demirci, Irmak İçen Taşkın, Aziz Paşahan, Meryem Rüveyda Sever, Yetkin Gök, Aydın Aktaş

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引用次数: 0

Abstract

Background: This work presents the synthesis of Ru(II)NHC complexes bearing a series of 4-fluorobenzyl group. These complexes have been characterized by a variety of spectroscopic methods (1H NMR, 13C NMR, and FTIR) and by elemental analysis techniques.

Methods: These complexes' antitumor activities against SH-SY5Y (human neuroblastoma) and HCT116 (human colon cancer) were investigated by 3-(4,5-dimethylthiazole-2-yl)-2,5-biphenyl tetrazolium bromide (MTT) assay.

Results: The results showed that all the synthesized complexes exhibited significant cytotoxic effect with low IC50 values 15 ± 0.57, 15.26 ± 0.71, 7.64 ± 0.30, 27.66 ± 0.36 and 14.45 ± 0.84 (μg/mL) respectively.

Conclusion: Furthermore, apoptosis assessed by double labeling with Annexin V-FITC/PI indicated that complexes 1b and 1d can effectively induce apoptosis and inhibit cell proliferation at the S phase in SH-SY5Y cells. Taken together, Ru(II)NHC complexes containing the 4- fluorobenzyl group have significant potential for the development of novel, highly effective anticancer agents.

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含氟基苯并咪唑功能化有机钌配合物的设计、合成、表征及抗肿瘤活性

背景：本文介绍了含一系列4-氟苯基的Ru(II)NHC配合物的合成。这些配合物已经通过各种光谱方法（1H NMR， 13C NMR和FTIR）和元素分析技术进行了表征。方法：采用3-（4,5-二甲基噻唑-2-基）-2,5-联苯溴化四氮唑（MTT）法检测这些配合物对SH-SY5Y（人神经母细胞瘤）和HCT116（人结肠癌）的抗肿瘤活性。结果：合成的配合物均表现出明显的细胞毒作用，IC50值分别为15±0.57、15.26±0.71、7.64±0.30、27.66±0.36、14.45±0.84 （μg/mL）。结论：进一步通过Annexin V-FITC/PI双标记评估SH-SY5Y细胞凋亡，复合物1b和1d能有效诱导SH-SY5Y细胞S期凋亡，抑制细胞增殖。综上所述，含有4-氟苯基的Ru(II)NHC配合物具有开发新型高效抗癌药物的巨大潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Medicinal Chemistry 医学-医药化学

CiteScore

4.30

自引率

4.30%

发文量

109

审稿时长

12 months

期刊介绍： Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.