13 results on '"Radik R. Shafikov"'
Search Results
2. Synthesis and Biological Evaluation of Novel Dispiro-Indolinones with Anticancer Activity
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Yan A. Ivanenkov, Maxim E. Kukushkin, Anastasia A. Beloglazkina, Radik R. Shafikov, Alexander A. Barashkin, Andrey A. Ayginin, Marina S. Serebryakova, Alexander G. Majouga, Dmitry A. Skvortsov, Viktor A. Tafeenko, and Elena K. Beloglazkina
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dispiro-indolinones ,MDM2 ,p53 ,PPI ,molecular docking ,cytotoxicity ,Organic chemistry ,QD241-441 - Abstract
Novel variously substituted thiohydantoin-based dispiro-indolinones were prepared using a regio- and diastereoselective synthetic route from 5-arylidene-2-thiohydantoins, isatines, and sarcosine. The obtained molecules were subsequently evaluated in vitro against the cancer cell lines LNCaP, PC3, HCTwt, and HCT(−/−). Several compounds demonstrated a relatively high cytotoxic activity vs. LNCaP cells (IC50 = 1.2–3.5 µM) and a reasonable selectivity index (SI = 3–10). Confocal microscopy revealed that the conjugate of propargyl-substituted dispiro-indolinone with the fluorescent dye Sulfo-Cy5-azide was mainly localized in the cytoplasm of HEK293 cells. P388-inoculated mice and HCT116-xenograft BALB/c nude mice were used to evaluate the anticancer activity of compound 29 in vivo. Particularly, the TGRI value for the P388 model was 93% at the final control timepoint. No mortality was registered among the population up to day 31 of the study. In the HCT116 xenograft model, the compound (170 mg/kg, i.p., o.d., 10 days) provided a T/C ratio close to 60% on day 8 after the treatment was completed. The therapeutic index—estimated as LD50/ED50—for compound 29 in mice was ≥2.5. Molecular docking studies were carried out to predict the possible binding modes of the examined molecules towards MDM2 as the feasible biological target. However, such a mechanism was not confirmed by Western blot data and, apparently, the synthesized compounds have a different mechanism of cytotoxic action.
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- 2023
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3. Optimization of the dipeptide motifs in the PSMA ligands linker structure: synthesis and in vitro evaluation
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Anastasiia A. Uspenskaya, Ekaterina A. Nimenko, Radik R. Shafikov, Nikolay Y. Zyk, Sergei A. Evteev, Natalia S. Dashkova, Yan A. Ivanenkov, Alexander G. Majouga, Dmitry A. Skvortsov, Anastasiia S. Garanina, Elena K. Beloglazkina, and Aleksei E. Machulkin
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Organic Chemistry ,General Pharmacology, Toxicology and Pharmaceutics - Published
- 2022
4. Influence of the dipeptide linker configuration on the activity of PSMA ligands
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Dmitry A. Skvortsov, Alexey E. Machulkin, Elena K. Beloglazkina, Stanislav A. Petrov, Alexander G. Majouga, Anastasiya A. Uspenskaya, Radik R. Shafikov, and Ekaterina A. Nimenko
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In vitro test ,Dipeptide ,010405 organic chemistry ,Stereochemistry ,Phenylalanine ,General Chemistry ,010402 general chemistry ,Cleavage (embryo) ,01 natural sciences ,0104 chemical sciences ,chemistry.chemical_compound ,chemistry ,Glutamate carboxypeptidase II ,Urea ,Tyrosine ,Linker - Abstract
Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in six steps by solid-phase synthesis. In vitro test for inhibiting the cleavage of N-acetylaspartylglutamate revealed the optimum linker containing l -phenylalanine in the structure on the N-terminus of a dipeptide chain.
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- 2020
5. Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom
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Nikolai Y. Zyk, Anton P. Ber, Ekaterina A. Nimenko, Radik R. Shafikov, Sergei A. Evteev, Stanislav A. Petrov, Anastasia A. Uspenskaya, Natalia S. Dashkova, Yan A. Ivanenkov, Dmitry A. Skvortsov, Elena K. Beloglazkina, Alexander G. Majouga, and Aleksei E. Machulkin
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Glutamate Carboxypeptidase II ,Male ,Nitrogen ,Lysine ,Organic Chemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Prostatic Neoplasms ,Ligands ,Biochemistry ,Cell Line, Tumor ,Drug Discovery ,Antigens, Surface ,Molecular Medicine ,Humans ,Molecular Biology - Abstract
We report an improved series of ligands targeting prostate specific membrane antigen (PSMA). The new compounds were designed by the introduction of changes in the structure of the aromatic fragment at ε-nitrogen atom of lysine that resulted in improved biological parameters. Some of them demonstrated high selectivity and nanomolar IC
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- 2022
6. Novel Copper-Containing Cytotoxic Agents Based on 2-Thioxoimidazolones
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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
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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.
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- 2020
7. PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation
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Vasilii Kolmogorov, Elena S. Khazanova, Yan A. Ivanenkov, Sergei V. Kovalev, Nikolay V. Zyk, Anastasia A. Uspenskaya, Alexander G. Majouga, Petr V. Gorelkin, Stanislav A. Petrov, Radik R. Shafikov, Anton P. Ber, Yulia A. Borisova, Dmitry A. Skvortsov, Ekaterina A. Nimenko, Vadim S. Pokrovsky, Elena K. Beloglazkina, Alexander Vaneev, Nikolay Y. Zyk, Alexander Erofeev, Alexander D. Khudyakov, Galina B. Smirnova, and Aleksei E. Machulkin
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Male ,Antineoplastic Agents ,Docetaxel ,Pharmacology ,urologic and male genital diseases ,Small Molecule Libraries ,Mice ,Structure-Activity Relationship ,Pharmacokinetics ,In vivo ,Cell Line, Tumor ,Drug Discovery ,medicine ,Glutamate carboxypeptidase II ,Distribution (pharmacology) ,Animals ,Humans ,MTT assay ,Rats, Wistar ,Cell Proliferation ,Mice, Inbred ICR ,Dose-Response Relationship, Drug ,Molecular Structure ,Chemistry ,Organic Chemistry ,General Medicine ,Neoplasms, Experimental ,Prostate-Specific Antigen ,Rats ,Drug delivery ,Rabbits ,Drug Screening Assays, Antitumor ,medicine.drug ,Conjugate - Abstract
Prostate cancer is one of the most commonly diagnosed men's cancers and remains one of the leading causes of cancer death. The development of approaches to the treatment of this oncological disease is an ongoing process. In this work, we have carried out the selection of ligands for the creation of conjugates based on the drug docetaxel and synthesized a series of three docetaxel conjugates. In vitro cytotoxicity of these molecules was evaluated using the MTT assay. Based on the assay results, we selected the conjugate which showed cytotoxic potential close to unmodified docetaxel. At the same time, the molar solubility of the resulting compound increased up to 20 times in comparison with the drug itself. In vivo evaluation on 22Rv1 (PSMA+) xenograft model demonstrated a good potency of the synthesized conjugate to inhibit tumor growth: the inhibition turned out to be more than 80% at a dose of 30 mg/kg. Pharmacokinetic parameters of conjugate distribution were analyzed. Also, it was found that PSMA-targeted docetaxel conjugate is less toxic than docetaxel itself, the decrease of molar acute toxicity in comparison with free docetaxel was up to 20%. Obtained conjugate PSMA-DOC is a good candidate for further expanded preclinical trials because of high antitumor activity, fewer side toxic effects and better solubility.
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- 2021
8. Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them
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Nikolay V. Zyk, Irina V. Saltykova, Anastasiya V Aladinskaya, Alexander Erofeev, Olga O. Krasnovskaya, Radik R. Shafikov, Elena K. Beloglazkina, Anastasiia S Garanina, Oleg Yu. Saveliev, Maxim A. Abakumov, Vladimir I. Polshakov, Ekaterina A. Nimenko, Yan A. Ivanenkov, Aleksei E. Machulkin, Olga A. Dontsova, Emil U Yamansarov, Alexander G. Majouga, Elena S. Khazanova, Anastasia A. Uspenskaya, Anton P. Ber, Galina B. Smirnova, Vadim S. Pokrovsky, Nikolay U. Zyk, Dmitry A. Skvortsov, Petr V. Gorelkin, Stanislav A. Petrov, A. V. Finko, and Rauf T Akhmirov
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Glutamate Carboxypeptidase II ,Male ,Cell Survival ,Transplantation, Heterologous ,Mice, Nude ,Antineoplastic Agents ,urologic and male genital diseases ,Ligands ,01 natural sciences ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,Structure-Activity Relationship ,Cell Line, Tumor ,Drug Discovery ,Glutamate carboxypeptidase II ,Aromatic amino acids ,Structure–activity relationship ,Animals ,Humans ,Tissue Distribution ,030304 developmental biology ,Fluorescent Dyes ,0303 health sciences ,Ligand ,Chemistry ,Optical Imaging ,Prostatic Neoplasms ,In vitro ,0104 chemical sciences ,Transplantation ,010404 medicinal & biomolecular chemistry ,Biochemistry ,Antigens, Surface ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Linker ,Conjugate - Abstract
Prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II (GCPII), is a suitable target for specific delivery of antitumor drugs and diagnostic agents due to its overexpression in prostate cancer cells. In the current work, we describe the design, synthesis, and biological evaluation of novel low-molecular PSMA ligands and conjugates with fluorescent dyes FAM-5, SulfoCy5, and SulfoCy7. In vitro evaluation of synthesized PSMA ligands on the activity of PSMA shows that the addition of aromatic amino acids into a linker structure leads to a significant increase in inhibition. The conjugates of the most potent ligand with FAM-5 as well as SulfoCy5 demonstrated high affinities to PSMA-expressing tumor cells in vitro. In vivo biodistribution in 22Rv1 xenografts in Balb/c nude mice of PSMA-SulfoCy5 and PSMA-SulfoCy7 conjugates with a novel PSMA ligand demonstrated good visualization of PSMA-expressing tumors. Also, the conjugate PSMA-SulfoCy7 demonstrated the absence of any explicit toxicity up to 87.9 mg/kg.
- Published
- 2021
9. New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity
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E. S. Yudina, Kseniya Yu. Vlasova, Dmitry A. Guk, A. S. Semkina, N. S. Dashkova, Alexander G. Majouga, V. P. Dyadchenko, Olga O. Krasnovskaya, Vladimir I. Pergushov, V. V. Shapovalov, Elena K. Beloglazkina, Nikolai V. Zyk, M. Ya. Mel’nikov, Dmitry A. Skvortsov, M. A. Kosarev, M. P. Rubtsova, Alexander V. Soldatov, Radik R. Shafikov, and A. A. Andreeva
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Metallocenes ,Alkyne ,Thio ,chemistry.chemical_element ,Antineoplastic Agents ,Apoptosis ,010402 general chemistry ,01 natural sciences ,Redox ,Cell Line ,Coordination complex ,Inorganic Chemistry ,Structure-Activity Relationship ,chemistry.chemical_compound ,Coordination Complexes ,Animals ,Humans ,DNA Cleavage ,Enzyme Inhibitors ,Telomerase ,Cell Proliferation ,chemistry.chemical_classification ,Dose-Response Relationship, Drug ,Molecular Structure ,010405 organic chemistry ,Imidazoles ,Serum Albumin, Bovine ,Combinatorial chemistry ,Copper ,Cycloaddition ,0104 chemical sciences ,HEK293 Cells ,Ferrocene ,chemistry ,Cattle ,Azide ,Drug Screening Assays, Antitumor - Abstract
Synthesis, characterization (HRMS, NMR, EPR, XANES, UV-Vis spectroscopy, and electrochemistry), DNA and BSA binding and in vitro biological screening of two new ferrocene-incorporated thiohydantoin derivatives (5 and 6) and their copper coordination compounds are reported. The ferrocene-based thiohydantoin derivatives were prepared by copper-catalyzed azide alkyne cycloaddition reactions between alkynyl ferrocenes and 5-(Z)-3-(2-azidoethyl)-2-(methylthio)-5-(pyridin-2-ylmethylene)-1H-imidazol-4H-one. Alkynyl ferrocenes necessary for these syntheses were prepared by new procedures. Intermolecular redox reactions between the ferrocene fragment and copper(+2) coordinated ions were studied by different methods to determine the mechanism and kinetic constants of redox processes. Ferrocene-containing imidazolones (5 and 6) and their copper complexes were also tested for their in vitro cytotoxic activity against MCF-7 and A-549 carcinoma cells, and also against the noncancerous cell line Hek-293. The results showed modest cytotoxicity against the subjected cancer cell line compared with cisplatin. The ability of the obtained compounds to cause DNA degradation and cell apoptosis was investigated, and the distribution of cytosol/pellets was studied by AAS.
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- 2018
10. Synthesis and biological evaluation of PSMA-targeting paclitaxel conjugates
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E. A. Plotnikova, Raisa I. Yakubovskaya, Nikolay U. Zyk, Yan A. Ivanenkov, Mikhail V. Kavalchuk, Elena K. Beloglazkina, Anastasia V. Aladinskaya, Alexander G. Majouga, Victor Koteliansky, Alexey E. Machulkin, Ekaterina A. Nimenko, Dmitry A. Skvortsov, Nikolay V. Zyk, Anton P. Ber, Radik R. Shafikov, and Anastasia A. Uspenskaya
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Male ,Paclitaxel ,Clinical Biochemistry ,Pharmaceutical Science ,01 natural sciences ,Biochemistry ,Prostate cancer ,chemistry.chemical_compound ,Mice ,Drug Delivery Systems ,Prostate ,Drug Discovery ,LNCaP ,medicine ,Glutamate carboxypeptidase II ,Animals ,Humans ,Cytotoxicity ,Molecular Biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Prostatic Neoplasms ,medicine.disease ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,medicine.anatomical_structure ,Targeted drug delivery ,Drug delivery ,Cancer research ,Molecular Medicine - Abstract
Prostate cancer (PC) is the second most commonly occurring cancer in men. Conventional chemotherapy has wide variety of disadvantages such as high systemic toxicity and low selectivity. Targeted drug delivery is a promising approach to decrease side effects of therapy. Prostate specific membrane antigen (PSMA) is overexpressed in prostate cancer cells while low level of expression is observed in normal cells. In this study we describe the development of Glu-urea-Lys based PSMA-targeting conjugates with paclitaxel. A series of new PSMA targeting conjugates with paclitaxel was designed and synthesized. The cytotoxicity of conjugates was evaluated against prostate (LNCaP, 22Rv1 and PC-3) and non-prostate (Hek293T, VA13, A549 and MCF-7) cell lines. The most promising conjugate 21 was examined in vivo using 22Rv1 xenograft mice model. It demonstrated good efficiency comparable with paclitaxel, while reduced toxicity. 3D molecular docking study was also performed to understand underlying mechanism of binding and further optimization of the linker substructure and conjugates structure for improving the target affinity. These conjugates may be useful for further design of novel PSMA targeting delivery systems for PC.
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- 2019
11. New copper(II) thiohydantoin complexes: Synthesis, characterization, and assessment of their interaction with bovine serum albumin and DNA
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Vladislav M Malinnikov, Anna V. Udina, Olga O. Krasnovskaya, Alexander G. Majouga, Mikhail A. Proskurnin, Dmitry A. Skvortsov, Vladimir A. Aladinskiy, Radik R. Shafikov, Nikolay V. Zyk, Elena K. Beloglazkina, Oleg I. Gromov, Dmitriy Guk, Ivan D. Sorokin, Ksenia Tishchenko, Marina Muratova, and Yan A. Ivanenkov
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Stereochemistry ,Supramolecular chemistry ,chemistry.chemical_element ,010402 general chemistry ,01 natural sciences ,Biochemistry ,Inorganic Chemistry ,chemistry.chemical_compound ,Coordination Complexes ,Animals ,Chelation ,Bovine serum albumin ,Quenching (fluorescence) ,biology ,010405 organic chemistry ,Serum Albumin, Bovine ,DNA ,Copper ,0104 chemical sciences ,chemistry ,Thiohydantoins ,Stability constants of complexes ,biology.protein ,Proton NMR ,Cattle ,Ethidium bromide ,Nuclear chemistry - Abstract
New copper(II) complexes of 2-alkylthio-5-arylmethylene-4H-imidazolin-4-ones: (5Z)-2-(methylsulfanyl)-3-(prop-2-en-1-yl)-5-(pyridin-2-ylmethylidene)-3,5-dihydro-4H-imidazol-4-one) ( 1a ), (5Z,5′Z)-2,2′-(ethan-1,2-diyldisulfanyldiyl)bis(5-(2-pyridilmethylen)-3-allyl-3,5-dihydo-4Н-imidazole-4-one) ( 2a ) and (5Z,5′Z)-3,3′-hexan-1,6-diylbis[5-(2-pyridilmethylen)-2-methylthiotetrahydro-4Н-imidazole-4-one)] ( 3a ) were synthesized as possible anticancer drugs. Their structures were characterized by 1 H NMR spectroscopy, elemental analysis, and X-ray crystallography. The composition of the complexes were found for 1a (Cu:L = 1 : 1 ), 2a (Cu:L = 2 : 1 ), and 3a (Cu:L = 2 : 1 ). The chelation constants were found by competitive complexation with ethylenediamine tetraacetate: 1a (6.7 ± 0.6) × 10 15 M − 1 , 2a = (4.9 ± 0.4) × 10 19 M − 2 , and 3a (5.7 ± 0.5) × 10 19 M − 2 . Supramolecular binding with calf thymus DNA by competitive ethidium bromide quenching was made for complex 2a as the most promising anticancer model, the Stern–Volmer constants were found to be K SV = (8.0 ± 0.4) × 10 6 M − 1 , K q = (6.5 ± 0.4) × 10 5 M − 1 . The binding of the complex 2a to BSA was made by the Scatchard method, the value of the constant is K b = (1.9 ± 0.2) × 10 6 M − 1 .
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- 2017
12. Correction: New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity
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M. P. Rubtsova, E. S. Yudina, Olga O. Krasnovskaya, Dmitry A. Guk, Nikolai V. Zyk, Elena K. Beloglazkina, M. A. Kosarev, Victor V. Shapovalov, M. Ya. Mel’nikov, Kseniya Yu. Vlasova, Alexander V. Soldatov, Radik R. Shafikov, Dmitriy A. Skvortsov, N. S. Dashkova, A. V. Andreeva, V. P. Dyadchenko, A. S. Semkina, A. G. Majouga, Anna A. Moiseeva, and Vladimir I. Pergushov
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Inorganic Chemistry ,chemistry.chemical_compound ,Ferrocene ,chemistry ,Thio ,chemistry.chemical_element ,Cytotoxicity ,Medicinal chemistry ,Copper - Abstract
Correction for ‘New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity’ by D. A. Guk et al., Dalton Trans., 2018, DOI: 10.1039/c8dt03164a.
- Published
- 2019
13. Synthesis and Biological Evaluation of S-, O- and Se-Containing Dispirooxindoles.
- Author
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Kukushkin M, Novotortsev V, Filatov V, Ivanenkov Y, Skvortsov D, Veselov M, Shafikov R, Moiseeva A, Zyk N, Majouga A, and Beloglazkina E
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- A549 Cells, Colorectal Neoplasms chemistry, Colorectal Neoplasms metabolism, Computer Simulation, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HCT116 Cells, HEK293 Cells, Humans, MCF-7 Cells, Male, Prostatic Neoplasms chemistry, Prostatic Neoplasms metabolism, Proto-Oncogene Proteins c-mdm2 chemistry, Proto-Oncogene Proteins c-mdm2 metabolism, Tumor Suppressor Protein p53 chemistry, Tumor Suppressor Protein p53 metabolism, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Colorectal Neoplasms drug therapy, Indoles chemical synthesis, Indoles chemistry, Indoles pharmacology, Prostatic Neoplasms drug therapy
- Abstract
A series of novel S-, O- and Se-containing dispirooxindole derivatives has been synthesized using 1,3-dipolar cycloaddition reaction of azomethine ylide generated from isatines and sarcosine at the double C=C bond of 5-indolidene-2-chalcogen-imidazolones (chalcogen was oxygen, sulfur or selenium). The cytotoxicity of these dispiro derivatives was evaluated in vitro using different tumor cell lines. Several molecules have demonstrated a considerable cytotoxicity against the panel and showed good selectivity towards colorectal carcinoma HCT116 p53
+/+ over HCT116 p53-/- cells. In particular, good results have been obtained for LNCaP prostate cell line. The performed in silico study has revealed MDM2/p53 interaction as one of the possible targets for the synthesized molecules. However, in contrast to selectivity revealed during the cell-based evaluation and the results obtained in computational study, no significant p53 activation using a reporter construction in p53wt A549 cell line was observed in a relevant concentration range.- Published
- 2021
- Full Text
- View/download PDF
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