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Future Med Chem ; 16(17): 1777-1789, 2024.
Article in English | MEDLINE | ID: mdl-39115052

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 IC50 = 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.


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Subject(s)
Antineoplastic Agents , Antioxidants , Cell Proliferation , Drug Design , Molecular Docking Simulation , Norfloxacin , Norfloxacin/pharmacology , Norfloxacin/chemical synthesis , Humans , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antioxidants/pharmacology , Antioxidants/chemical synthesis , Antioxidants/chemistry , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , HeLa Cells , Cell Survival/drug effects , Structure-Activity Relationship , Molecular Structure
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