1. Comparative in vitro Studies of the Topoisomerase I Inhibition and Anticancer Activities of Metallated N‐Confused Porphyrins and Metallated Porphyrins
- Author
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Usein M. Dzhemilev, Nyancy Halder, Harapriya Rath, Vladimir A. D’yakonov, Ilfir R. Ramazanov, and Lilya U. Dzhemileva
- Subjects
Metalloporphyrins ,Stereochemistry ,Kinetics ,Antineoplastic Agents ,Apoptosis ,Topoisomerase-I Inhibitor ,01 natural sciences ,Biochemistry ,Jurkat cells ,HeLa ,Cell Line, Tumor ,Drug Discovery ,polycyclic compounds ,Humans ,heterocyclic compounds ,General Pharmacology, Toxicology and Pharmaceutics ,Cell Proliferation ,Pharmacology ,Molecular Structure ,biology ,010405 organic chemistry ,Chemistry ,Topoisomerase ,Cell Cycle ,Organic Chemistry ,Cell cycle ,biology.organism_classification ,In vitro ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,DNA Topoisomerases, Type I ,biology.protein ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Topoisomerase I Inhibitors ,DNA Damage - Abstract
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.
- Published
- 2020