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通过计算机模拟、体外实验和DNA切口实验评估合成的新型铱(III)配合物对HeLa细胞系的作用

Evaluation of the Synthesized Novel Iridium (III) Complexes Against HeLa Cell Lines Through In-Silico, In-Vitro and DNA Nicking.

作者信息

Priyadarshini G Sathya, Muthusankar Aathi, Subramani Ramesh, Gopal Selvi

机构信息

Department of Chemistry, PSGR Krishnammal College for Women, Peelamedu, Coimbatore, India.

Protein Biology Group, International Centre for Genetic Engineering and Biotechnology, New Delhi 110067, India.

出版信息

Asian Pac J Cancer Prev. 2021 Feb 1;22(2):447-455. doi: 10.31557/APJCP.2021.22.2.447.

Abstract

Globally, the pharmaceutical industry is continuously driven in search of new anticancer drugs due to increasing rate of cancer patients. Clinical trials of Cisplatin has been explored, however, usage of Cisplatin as a drug is limited due to its various side effects, hence, alternative to platinum based complex drugs and its analogues are needed. Iridium complexes have been attracted widespread interests by virtue of their pharmacological and photo-physical properties; however the less number of complexes was reported in the literature. In this article, a new series of novel Iridium (III) complexes were synthesized using substituted quinoline Schiff Base (SB) ligands and characterized by spectroscopic techniques. The in- vitro cyto-toxicity assay showed that the Iridium (III) complex activity is equal to standard Cisplatin. In addition, computational docking studies have shown that the prominent binding sites for synthesized complexes against HeLa cell lines, which is comparable with standard Cisplatin drugs and other Ruthenium complexes.
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摘要

在全球范围内,由于癌症患者数量不断增加,制药行业一直在不断推动寻找新的抗癌药物。顺铂的临床试验已经展开,然而,由于顺铂存在各种副作用,其作为药物的使用受到限制,因此,需要铂基复合药物及其类似物的替代品。铱配合物凭借其药理和光物理性质引起了广泛关注;然而,文献中报道的配合物数量较少。在本文中,使用取代喹啉席夫碱(SB)配体合成了一系列新型铱(III)配合物,并通过光谱技术对其进行了表征。体外细胞毒性试验表明,铱(III)配合物的活性与标准顺铂相当。此外,计算对接研究表明,合成配合物与HeLa细胞系的主要结合位点,与标准顺铂药物和其他钌配合物相当。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4def/8190364/3c12044ab0cd/APJCP-22-447-g001.jpg

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