A5069914829- Estrogen and related hormone effects
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and biological activity
- Bioactive Compounds and Antitumor Agents
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- PI3K/AKT/mTOR signaling in cancer
- Cancer, Hypoxia, and Metabolism
- MicroRNA in disease regulation
- Natural product bioactivities and synthesis
- Cancer-related Molecular Pathways
- Computational Drug Discovery Methods
- Cancer Cells and Metastasis
- Steroid Chemistry and Biochemistry
- Cancer-related molecular mechanisms research
- Extracellular vesicles in disease
- NF-κB Signaling Pathways
- Enzyme function and inhibition
- Synthesis and Reactions of Organic Compounds
- Cytokine Signaling Pathways and Interactions
- Click Chemistry and Applications
- Metabolism, Diabetes, and Cancer
- RNA Interference and Gene Delivery
- Cancer Immunotherapy and Biomarkers
Gause Institute of New Antibiotics Russian Academy of Medical Sciences
2024-2025
N. I. Lobachevsky State University of Nizhny Novgorod
2023-2024
Russian Cancer Research Center NN Blokhin
2015-2024
Ministry of Health of the Russian Federation
2016-2024
National Medical Research Center of Cardiology
2019-2022
Ministry of Health
2021
Institute of Oncology NN Petrov
2017
Academy of Medical Sciences
2010-2013
Russian Academy of Sciences
2008-2013
The promising antitumor effects of progesterone derivatives have been identified in many studies. However, the specific mechanism action this class compounds has not fully described. Therefore, study, we investigated antiproliferative and (anti)estrogenic activities novel pentacyclic benzylidenes series. were evaluated on hormone-dependent MCF7 breast cancer cells using MTT test. Estrogen receptor α (ERα) activity was assessed by a luciferase-based reporter assay. Immunoblotting used to...
Metformin, a biguanide antidiabetic drug, is used to decrease hyperglycemia in patients with type 2 diabetes. Recently, the epidemiological studies revealed potential of metformin as an anti-tumor drug for several types cancer, including breast cancer. Anti-tumor action was found be mediated, at least part, via activation adenosine monophosphate-activated protein kinase (AMPK)—intracellular energy sensor, which inhibits mammalian target rapamycin (mTOR) and some other signaling pathways....
Exosomes are small vesicles which produced by the cells and released into surrounding space. They can transfer biomolecules recipient cells. The main goal of work was to study exosome involvement in cell hormonal resistance. experiments were performed on vitro cultured estrogen-dependent MCF-7 breast cancer sublines resistant SERM tamoxifen and/or biguanide metformin, exerts its anti-proliferative effect, at least a part, via suppression estrogen machinery. exosomes purified differential...
Most breast and prostate tumors are hormone-dependent, making it possible to use hormone therapy in patients with these tumors. The design of effective endocrine drugs that block the growth have no severe side effects is a challenge. Thereupon, synthetic steroids promising therapeutic for treatment diseases such as hormone-dependent cancers. Here, we describe novel series steroidal pyrimidines dihydrotriazines anticancer activities. A flexible approach unknown pyrimidine dihydrotriazine...
Phytoestrogens are a group of plant-derived compounds with an estrogen-like activity. In mammalians, phytoestrogens bind to the estrogen receptor (ER) and participate in regulation cell growth gene transcription. There several reports cytotoxic effects different cancer lines. The aim this study was measure phytoestrogen activity against breast cells levels ER expression elucidate molecular pathways regulated by leader compound. Methods used include immunoblotting, transfection luciferase...
The loss of hormonal dependency breast tumor cells is often accompanied with the appearance epithelial-mesenchymal transition (EMT) features and increase in cell metastasis invasiveness. central role EMT belongs to transcription factors Snail responded for decrease E-cadherin expression contacts, stimulation mobility Aim was study relationships between estrogen receptor machinery Snail1 signaling, mechanism regulation hormone-resistant cancer cells. experiments were performed on...
Cytotoxic effects against breast cancer cells.
Aim: The study aims to analyze the effect of long-term incubation ERα-positive MCF7 breast cancer cells with 4-hydroxytamoxifen (HT) on their sensitivity tubulin polymerization inhibitor docetaxel. Methods: analysis cell viability was performed by MTT method. expression signaling proteins analyzed immunoblotting and flow cytometry. ERα activity evaluated gene reporter assay. To establish hormone-resistant subline MCF7, were treated for 12 months. Results: developed MCF7/HT has lost...
Novel N-(4,5,6,7-tetrahydrobenzisoxazol-4-yl)amide derivatives were designed and synthesized as potential HSP90 inhibitors. The synthetic pathway commenced with 6,7-dihydrobenzo[d]isoxazol-4(5H)-ones, utilizing the Ritter reaction a key step. Molecular docking, molecular dynamics simulations, MM/GBSA analysis guided selection of compounds for synthesis provided insights into interaction mode most active compound HSP90α. exhibited significant antiproliferative effects against breast cancer...
An efficient and practical method has been developed for the synthesis of steroidal imidazoheterocycles via cost-effective environmentally benign FeCl3-catalyzed oxidative amination. A library imidazo[1,2-a]pyridines was directly synthesized from readily available 2-aminopyridines ketones in aerobic conditions. The compounds were screened activity on human microsomal cytochrome P450s CYP7, CYP17 CYP21. Antiproliferative two lead 3ia 3la additionally evaluated against MCF-7 (breast cancer),...
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...
Secoisolariciresinol diglucoside (SDG) is isolated from Linum usitatissimum seeds. The antiproliferative effects of SDG (1) and its derivatives secoisolariciresinol (2) secoisolariciresinol-4', 4″-diacetate (3) have been evaluated on MCF-7 breast cancer cells normal epithelial line MCF-10A. Lignan 1 has not shown cytotoxic cells, while 2 3 inhibited cell growth with IC50 values 25 11 µM, respectively. Estrogen receptor alpha a key driver in cells. Compound did affect the activity ERα, showed...
Essential oils (EOs) are known for their use in cosmetics, food industries, and traditional medicine. This study presents the chemical composition therapeutic properties against kinetoplastid eukaryotic cells of EO from Melaleucaleucadendra (L.) L. (Myrtaceae). Forty-five compounds were identified oil by GC-MS, containing a major component 1,8-cineole (61%). The inhibits growth Leishmania amazonensis Trypanosoma brucei at IC50 values <10 μg/mL. However, 1,8 cineole was not main compound...
Local targeted "inside-out" hyperthermia of tumors via nanoparticles is able to sensitize tumor cells chemotherapy, radiation therapy, gene immunotherapy, or other effects, significantly reducing the duration and intensity treatment. In this article, new nanomaterials are proposed be used as anticancer agents: boron-doped nanodiamonds with sizes about 10 nm synthesized for first time by high-temperature high-pressure (HTHP) method. The heating ability was investigated under different...