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Comparative in vitro Studies of the Topoisomerase I Inhibition and Anticancer Activities of Metallated N-Confused Porphyrins and Metallated Porphyrins.
ChemMedChem ( IF 3.4 ) Pub Date : 2020-03-18 , DOI: 10.1002/cmdc.201900633
Nyancy Halder 1 , Lilya U Dzhemileva 2 , Ilfir R Ramazanov 2 , Vladimir A D'yakonov 2 , Usein M Dzhemilev 2 , Harapriya Rath 1
Affiliation  

Using the original approach, a series of metallated N‐confused porphyrins and metallated porphyrins have been synthesized and characterized. For all the synthesized porphyrins, in vitro studies of cytotoxic activity against K562, U937, HL‐60, Jurkat, A549 and HeLa cancer cell lines, the ability to induce apoptosis and effects on the cell cycle as well as the kinetics of proliferative activity of porphyrins and their respective metallated complexes in real time have been developed. The inhibitory activity of metallated porphyrins against human topoisomerase I and the possible mechanism of inhibition have been carried out by modelling using molecular docking.

中文翻译:

金属化的N混淆卟啉和金属化的卟啉对拓扑异构酶I抑制和抗癌活性的体外比较研究。

使用原始方法,已合成和表征了一系列金属化的N混淆卟啉和金属化的卟啉。对于所有的合成卟啉,在体外对K562,U937,HL-60,的Jurkat,A549和HeLa癌细胞系,以诱导细胞凋亡和效果对细胞周期以及增殖活性的动力学的能力的细胞毒活性的研究实时开发了卟啉及其各自的金属化配合物。金属化卟啉对人拓扑异构酶I的抑制活性和可能的​​抑制机理已通过分子对接建模进行了研究。
更新日期:2020-03-19
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