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Design, synthesis and evaluation of novel norfloxacin analogs as potent anticancer and antioxidant agents.

Authors :
Qurban F
Shahzad SA
Khaskheli MS
Khan SU
Khan SA
Rauf W
Islam S
Mannan A
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.

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