A5039767113- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis of Organic Compounds
- Synthesis and Biological Evaluation
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Chemical Synthesis and Analysis
- Catalytic Cross-Coupling Reactions
- Photodynamic Therapy Research Studies
- Cancer therapeutics and mechanisms
- Nanoplatforms for cancer theranostics
- Bioactive Compounds and Antitumor Agents
- Synthesis and Biological Activity
- Synthetic Organic Chemistry Methods
- Porphyrin and Phthalocyanine Chemistry
- Catalytic C–H Functionalization Methods
- Chemical Synthesis and Reactions
- Synthesis of heterocyclic compounds
- Carbohydrate Chemistry and Synthesis
- Sulfur-Based Synthesis Techniques
- Synthesis and Catalytic Reactions
- Coordination Chemistry and Organometallics
- Glycosylation and Glycoproteins Research
- Organometallic Complex Synthesis and Catalysis
- Nanoparticle-Based Drug Delivery
N. I. Lobachevsky State University of Nizhny Novgorod
2016-2025
Yaroslav-the-Wise Novgorod State University
2015-2024
Saratov State University
2002-2022
N.D. Zelinsky Institute of Organic Chemistry
2022
University of Cologne
2012-2019
Nizhny Novgorod State Pedagogical University
2003-2015
Nizhny Novgorod Research Institute of Traumatology and Orthopedics
2015
Ludwig-Maximilians-Universität München
2012
Lomonosov Moscow State University
2005-2010
Centre National de la Recherche Scientifique
1999-2007
The review discusses the latest advances in directed synthesis and application of macroheterocyclic compounds science, engineering technology, viz.as catalysts for various processes photo-and electrocatalysis, optical chemosensors metal cations, selective receptors organic compounds, inductors selectors, nonlinear optics, electronics, as magnets, photosensitizers PDT a number oncological diseases antimicrobial PDT, etc.
The chemistry of heterocyclic compounds has traditionally been and remains a bright area chemical science in Russia. This is due to the fact that many heterocycles find widest application. These are key structural fragments most drugs, plant protection agents. Many natural also derivatives heterocycles. At present, more than half hundreds millions known collective review devoted achievements Russian chemists this field over last 15–20 years. presents leading heterocyclists representing both...
A series of A-ring variously methoxylated 4-(3-hydroxy-4-methoxyphenyl)coumarins related to combretastatin A-4 was prepared by cross-coupling reactions. Cytotoxicity studies indicated a potent activity against HBL100 cell line. Substitution patterns on had only slight effect antiproliferative activity. For most cytotoxic compounds, the as potential modulators P-gp and BCRP efflux pumps evaluated. The results show that compounds 2 7 were able restore mitoxantrone accumulation (BCRP) at...
A midthroughput screening follow-up program targeting the first bromodomain of human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This compound binds with affinity in low micromolar range yet exerts suitable unexpected selectivity vitro against other members and extra-terminal domain (BET) family. structure-based pinpointed a role ZA loop, paving way for development potent selective BET-BRDi probes.
Over the past few decades, hit identification has been greatly facilitated by advances in high-throughput and fragment-based screenings. One major hurdle remaining drug discovery is process automation of hit-to-lead (H2L) optimization. Here, we report a time- cost-efficient integrated strategy for H2L optimization as well partially automated design potent chemical probes consisting focused-chemical-library virtual screening coupled with robotic diversity-oriented de novo synthesis vitro...
Copper-catalyzed O- and N-arylation reactions involving triarylbismuth diacetates or aryllead triacetates are ligand coupling which were discovered in the eighties independently by Bartons Dodonovs groups. These reagents lead generally to efficient arylation under mild neutral conditions (room temperature 40 dgree C, no added basic reagent). Recently, scope of these main group metal mediated was broadened when Chan Evans reported that organoboron compounds can be used as source organic aryl...
A new water-soluble conjugate, consisting of a chlorin-e6 photosensitizer part, 4-arylaminoquinazoline moiety with affinity to epidermal growth factor receptors, and hydrophilic β-d-maltose fragment, was synthesized starting from methylpheophorbide-a in seven steps. The prepared conjugate exhibited low levels dark cytotoxicity pronounced photoinduced at submicromolar concentrations vitro, an IC50(dark)/IC50(light) ratio ∼368 singlet oxygen quantum yield about 20%. In tumor-bearing Balb/c...
In this report, we developed novel chlorin/arylaminoquinazoline conjugates for targeted photodynamic therapy of cancer. The synthesized photosensitizers consisted chlorin-
A series of conformationally flexible furan-derived allocolchicinoids was prepared from commercially available colchicine in good to excellent yields using a three-step reaction sequence. Cytotoxicity studies indicated the potent activity two compounds against human epithelial and lymphoid cell lines (AsPC-1, HEK293, Jurkat) as well Wnt-1 related murine line W1308. The results vitro experiments demonstrated that major effect these induction cycle arrest G2/M phase direct consequence...
Published data on the stereo- and enantioselective synthesis of allocolchicinoids, which are interest as antitumour agents, summarized. The stereochemistry these compounds is described. Two key approaches to their preparation considered, namely, from natural colchicine total commercially available reagents. Various syntheses N-acetylcolchicinol performed using biaryl oxidative reductive coupling, cyclopropanation–ring expansion Nicholas reaction. synthetic routes allocolchicine based...
A (series) range of potential dimorpholinoquinazoline-based inhibitors the PI3K/Akt/mTOR cascade was synthesized. Several compounds exhibited cytotoxicity towards a panel cancer cell lines in low and sub-micromolar range. Compound 7c with highest activity moderate selectivity MCF7 cells which express mutant type PI3K also tested for ability to inhibit PI3K-(signaling pathway) downstream effectors associated proteins. inhibited phosphorylation Akt, mTOR, S6K at 125-250 nM. It triggered PARP1...
(1) Background: This investigation aimed at developing a series of c-Met-targeting cabozantinib-based PROTACs. (2) Methods: Purification intermediate and target compounds was performed using column chromatography, in vitro antiproliferation activity measured standard MTT assay c-Met degradation via the immunoblotting technique. (3) Results: Several exhibited antiproliferative towards different cell lines breast cancer (T47D, MDA-MB-231, SKBR3, HCC1954 MCF7) same level as parent cabozantinib...
Abstract A series of novel pyrrolo‐allocolchicine derivatives (containing a 1‐methyl‐1 H ‐indol‐5‐yl moiety replacing ring C) was synthesized. The tetracyclic system constructed by Suzuki–Miyaura cross‐coupling 1‐methylindole‐5‐boronate with an ortho ‐iodo‐dihydrocinnamic acid derivative and subsequent intramolecular Friedel–Crafts acylation. After reduction the resulting ketone, nitrogen functionality introduced in Mitsunobu‐type reaction using zinc azide followed LiAlH 4 reduction....
Reliable procedures for the preparation of azides derived from colchicine (1), allocolchicine (3) and N-acetylcolchinol (4a) were developed.These then employed in Cu-catalyzed Huisgen-Sharpless [3+2] cycloaddition ("click") reactions with alkynes under microwave irradiation.The method developed opens a convenient efficient access to libraries new C-7-modified colchicinoids (triazole derivatives).In addition, plausible mechanistic rationale colchicine-allocolchicine rearrangement is suggested.