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Design, synthesis and evaluation of novel norfloxacin analogs as potent anticancer and antioxidant agents.
- Source :
-
Future medicinal chemistry [Future Med Chem] 2024; Vol. 16 (17), pp. 1777-1789. Date of Electronic Publication: 2024 Aug 08. - Publication Year :
- 2024
-
Abstract
- Aim: To synthesize a novel series of norfloxacin analogs and to evaluate biological activity. Methodology: Novel norfloxacin analogs were synthesized and characterized by NMR and mass spectrometry. Antiproliferative and antioxidant properties were studied. Results: Compound 2f was the most potent against HeLa cell-line with 100% inhibition of cell viability IC <subscript>50</subscript>  = 3.1 ± 0.2 μM. All compounds exhibit moderate to excellent antioxidant properties. Docking study demonstrates higher binding affinity of compounds with respective anticancer (B-cell lymphoma-2) and (tyrosinase) antioxidant targets. In silico absorption, distribution, metabolism and excretion profile of compounds proves all synthesized compounds follow Lipinski's rule of drug likeness, non toxic and possess passive gastrointestinal absorption. Conclusion: The biological profile suggest that the synthesized norfloxacin analogs can be a novel scaffold for future anticancer drug development.
- Subjects :
- Humans
Drug Screening Assays, Antitumor
HeLa Cells
Cell Survival drug effects
Structure-Activity Relationship
Molecular Structure
Norfloxacin pharmacology
Norfloxacin chemical synthesis
Antineoplastic Agents pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Drug Design
Antioxidants pharmacology
Antioxidants chemical synthesis
Antioxidants chemistry
Cell Proliferation drug effects
Molecular Docking Simulation
Subjects
Details
- Language :
- English
- ISSN :
- 1756-8927
- Volume :
- 16
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Future medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 39115052
- Full Text :
- https://doi.org/10.1080/17568919.2024.2383165