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Your search keyword '"Vita N. Nikitina"' showing total 2 results
Start Over Author "Vita N. Nikitina" Journal journal of medicinal chemistry
2 results on '"Vita N. Nikitina"'

1. Pt(IV) Prodrugs with Non-Steroidal Anti-inflammatory Drugs in the Axial Position

Author

Daniil V. Spector, Kirill G. Pavlov, Roman A. Akasov, Alexander N. Vaneev, Alexander S. Erofeev, Petr V. Gorelkin, Vita N. Nikitina, Elena V. Lopatukhina, Alevtina S. Semkina, Kseniya Yu. Vlasova, Dmitrii A. Skvortsov, Vitaly A. Roznyatovsky, Nikolay V. Ul’yanovskiy, Ilya I. Pikovskoi, Sergey A. Sypalov, Anastasiia S. Garanina, Stepan S. Vodopyanov, Maxim A. Abakumov, Yulia L. Volodina, Alina A. Markova, Albina S. Petrova, Dmitrii M. Mazur, Dmitry A. Sakharov, Nikolay V. Zyk, Elena K. Beloglazkina, Alexander G. Majouga, and Olga O. Krasnovskaya

Subjects
Mice, Inbred BALB C, Anti-Inflammatory Agents, Non-Steroidal, Antineoplastic Agents, Platinum Compounds, Mice, Cell Line, Tumor, Drug Design, Drug Discovery, MCF-7 Cells, Animals, Humans, Molecular Medicine, Prodrugs, Cisplatin
Abstract

We report herein the design, synthesis, and biological investigation of a series of novel Pt(IV) prodrugs with non-steroidal anti-inflammatory drugs naproxen, diclofenac, and flurbiprofen, as well as these with stearic acid in the axial position. Six Pt(IV) prodrugs

Published
2022

2. Novel Copper-Containing Cytotoxic Agents Based on 2-Thioxoimidazolones

Author

Nikolay V. Zyk, Dmitry A Sakharov, Dmitry A. Guk, Vita N. Nikitina, Alexander Erofeev, Dmitrii M. Mazur, Vadim S. Pokrovsky, Anna A. Moiseeva, Alexey E Naumov, Petr V. Gorelkin, Mikhail A. Soldatov, Roman Akasov, Alexander G. Majouga, Victor V. Shapovalov, A. S. Semkina, Mikhail Ya. Melnikov, Irina V Zhirkina, Olga O. Krasnovskaya, Elena K. Beloglazkina, Vladimir I. Pergushov, Viktor A. Tafeenko, Kseniya Yu. Vlasova, Dmitry A. Skvortsov, Saida S Karshieva, Oksana O Ryabaya, Alexander V. Soldatov, Radik R. Shafikov, Vasily M. Gerasimov, and Alexander Vaneev

Subjects
DNA damage, Molecular Conformation, chemistry.chemical_element, Antineoplastic Agents, Apoptosis, Crystallography, X-Ray, Ligands, Models, Biological, 01 natural sciences, Redox, Coordination complex, Metal, Structure-Activity Relationship, 03 medical and health sciences, Coordination Complexes, Spheroids, Cellular, Drug Discovery, Humans, Structure–activity relationship, Cytotoxicity, Telomerase, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Chemistry, Imidazoles, Copper, Combinatorial chemistry, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, DNA Intercalation, visual_art, MCF-7 Cells, visual_art.visual_art_medium, Molecular Medicine, Reactive Oxygen Species, Oxidation-Reduction, DNA Damage
Abstract

A series of 73 ligands and 73 of their Cu+2 and Cu+1 copper complexes with different geometries, oxidation states of the metal, and redox activities were synthesized and characterized. The aim of the study was to establish the structure-activity relationship within a series of analogues with different substituents at the N(3) position, which govern the redox potentials of the Cu+2/Cu+1 redox couples, ROS generation ability, and intracellular accumulation. Possible cytotoxicity mechanisms, such as DNA damage, DNA intercalation, telomerase inhibition, and apoptosis induction, have been investigated. ROS formation in MCF-7 cells and three-dimensional (3D) spheroids was proven using the Pt-nanoelectrode. Drug accumulation and ROS formation at 40-60 μm spheroid depths were found to be the key factors for the drug efficacy in the 3D tumor model, governed by the Cu+2/Cu+1 redox potential. A nontoxic in vivo single-dose evaluation for two binuclear mixed-valence Cu+1/Cu+2 redox-active coordination compounds, 72k and 61k, was conducted.

Published
2020

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