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Rational Design and Synthesis of Isatin-Chalcone Hybrids Integrated with 1H-1,2,3-Triazole: Anti-Proliferative Profiling and Molecular Docking Insights.
- Source :
-
ChemMedChem [ChemMedChem] 2024 Jul 15; Vol. 19 (14), pp. e202400015. Date of Electronic Publication: 2024 May 22. - Publication Year :
- 2024
-
Abstract
- In this study, a series of isatin-chalcone linked triazoles were synthesized using Cu-promoted Azide-Alkyne Cycloaddition (CuAAC) reaction and evaluated for their cytotoxicity against various cancer cell lines. The most potent compound displayed approximately 2.5 times greater activity compared to both reference compounds against ovarian cancer cell lines. These findings were supported by caspase-mediated apoptosis and molecular docking analyses. Docking revealed comparable VEGFR-2 affinities for 5 b and 5-FU but highlighted stronger interaction of 5 b with EGFR, evident from its lower docking score. Overall, these results signify the notable anti-proliferative potential of most synthesized hybrids, notably emphasizing the efficacy of compound 5 b in suppressing cancer cell growth.<br /> (© 2024 Wiley-VCH GmbH.)
- Subjects :
- Humans
Structure-Activity Relationship
Cell Line, Tumor
Chalcone chemistry
Chalcone pharmacology
Chalcone chemical synthesis
Molecular Structure
Apoptosis drug effects
Dose-Response Relationship, Drug
Chalcones chemistry
Chalcones pharmacology
Chalcones chemical synthesis
Vascular Endothelial Growth Factor Receptor-2 antagonists & inhibitors
Vascular Endothelial Growth Factor Receptor-2 metabolism
Triazoles chemistry
Triazoles pharmacology
Triazoles chemical synthesis
Molecular Docking Simulation
Isatin chemistry
Isatin pharmacology
Drug Design
Cell Proliferation drug effects
Antineoplastic Agents pharmacology
Antineoplastic Agents chemistry
Antineoplastic Agents chemical synthesis
Drug Screening Assays, Antitumor
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 19
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 38638026
- Full Text :
- https://doi.org/10.1002/cmdc.202400015