A5084867717- Synthesis and biological activity
- Bioactive Compounds and Antitumor Agents
- Genomics, phytochemicals, and oxidative stress
- X-ray Diffraction in Crystallography
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- Quinazolinone synthesis and applications
- Breast Lesions and Carcinomas
- Medical Imaging and Pathology Studies
- Radiomics and Machine Learning in Medical Imaging
- Natural product bioactivities and synthesis
- Radiopharmaceutical Chemistry and Applications
- Click Chemistry and Applications
- Garlic and Onion Studies
- Cancer Diagnosis and Treatment
- Histiocytic Disorders and Treatments
- Alzheimer's disease research and treatments
- Vascular Tumors and Angiosarcomas
- Cancer Research and Treatment
- Nonlinear Optical Materials Research
- Mathematical Biology Tumor Growth
- Multicomponent Synthesis of Heterocycles
- Cancer and biochemical research
- Dermatological and COVID-19 studies
University of Pavol Jozef Šafárik
2014-2024
Institute of Chemistry of the Slovak Academy of Sciences
2018-2024
University of Veterinary Medicine in Košice
2018-2021
Although new chemotherapy significantly increased the survival of breast cancer (BC) patients, use these drugs is often associated with serious toxicity. The discovery novel anticancer agents for BC therapy expected. This study was conducted to explore antiproliferative effect newly synthesized indole chalcone derivative ZK-CH-11d on human cell lines. MTT screening, flow cytometry, Western blot, and fluorescence microscopy were used evaluate mode death. suppressed proliferation cells minimal...
The synthesis, anticancer, and antioxidant activities of a series indole-derived hybrid chalcones are reported here. First, using the well-known Claisen-Schmidt condensation method, set 29 has been designed, synthesized, consequently characterized. Subsequently, screening for antiproliferative activity synthesized was performed on five cancer cell lines (HCT116, HeLa, Jurkat, MDA-MB-231, MCF7) two non-cancer (MCF-10A Bj-5ta). Chalcone 18c, bearing 1-methoxyindole catechol structural...
The synthesis, anticancer and antioxidant activity of a series indole-derived hybrid chalcones are reported here. First, using well known Claisen-Schmidt condensation method set 29 has been designed, synthesized, consequently characterized. Subsequently, screening for the antiproliferative synthesized was performed on five cancer (HCT116, HeLa, Jurkat, MDA-MB-231 MCF7) two non-cancer (MCF-10A Bj-5ta) cell lines. Chalcone 18c bearing 1-methoxyindole catechol structural features, exhibited...
Performing solution-phase oximation reactions with hydroxylamine hydrochloride (NH2OH·HCl) carries significant risk, especially in aqueous solutions. In the present study, four N-substituted indole-3-carboxaldehyde oximes were prepared from corresponding aldehydes by solvent-free reaction NH2OH·HCl and a base (NaOH or Na2CO3) using mechanochemical approach, thus minimizing possible risk. all cases, conversion to was almost complete. The focus of this work is on...
This study was focused on investigating the antiproliferative effects of chalcone hybrids in melanoma cancer cells. Among seven hybrids, chalcone-acridine hybrid 1C most potent and selected for further mechanism studies. vitro revealed effect via cell cycle arrest apoptosis induction. Cell at G2/M phase associated with modulation expression or phosphorylation specific cycle-associated proteins (cyclin B1, p21, ChK1), tubulins, as well activation DNA damage response pathway. Chalcone also...
Over the past decades, natural products have emerged as promising agents with multiple biological activities. Many studies suggest antioxidant, antiangiogenic, antiproliferative and anticancer effects of chalcones their derivatives. Based on these findings, we decided to evaluate newly synthetized chalcone L1 in a human cervical carcinoma cell (HeLa) model. Presented results were obtained by western blot flow cytometric analyses, live imaging antimigratory potential HeLa cells was...
This study focuses on the synthesis and structural characterization of new compounds that integrate thiazolidine-2,4-dione, acridine moiety, an acetamide linker, aiming to leverage synergistic effects these pharmacophores for enhanced therapeutic potential. The newly designed molecules were efficiently synthesized through a multi-step process subsequently transformed into their hydrochloride salts. Comprehensive spectroscopic techniques, including nuclear magnetic resonance (NMR),...
An efficient eco-friendly one-step mechanochemical synthesis of indole hybrid chalcones via the Claisen–Schmidt condensation 1-methylindole-3-carboxaldehyde with various substituted acetophenones is described using liquid assisted grinding in a high-energy ball mill. The notable advantages present method are small organic solvent required (100 μL ethanol) and mainly shorter reaction time (15–60 min) as compared to conventional method. Antiproliferative activity synthesized was studied on...
The authors report on the synthesis and biological evaluation of new compounds whose structure combines tacrine indole moieties. Tacrine-indole heterodimers were designed to inhibit cholinesterases β-amyloid formation, cross blood-brain barrier. most potent acetylcholinesterase inhibitors 3c 4d (IC50 = 25 39 nM, respectively). Compound displayed considerably higher selectivity for relative human plasma butyrylcholinesterase in comparison compound (selectivity index: IC50...
Derivatives combining acridine, pyrrole, and thiazolidine rings have emerged as promising candidates in the field of antitumor drug discovery. This paper aims to highlight importance these three structural motifs developing potent selective anticancer agents. The integration within a single molecule offers potential for synergistic effects, targeting multiple pathways involved tumor growth progression. Spiro derivatives were efficiently synthesized two-step process starting from...
Backgroud: Antiproliferative activity of chalcones against various cancer cells was documented. Aim this work to investigate mechanism antiproliferative effect synthetic on human colorectal cells.