Novel amodiaquine analogues to treat cervical cancer and microbial infection in the future
Aim: To synthesize and explore the therapeutic potential of amodiaquine analogues. Methodology: New promising analogues were synthesized by nucleophilic substitution at the 4-amino position and were characterized using 1H NMR, 13C NMR and FT-IR spectroscopic techniques. Results: Antibacterial and cytotoxic screening revealed the high potency of these compounds; analogue AS1 had an 34.3 ± 0.18 mm zone of inhibition against Pseudomonas aeruginosa. Excellent activity against fungal strains, that is, Candida albicans (39.6 ± 0.23 mm) was shown by analogue AS2. Analogue AS1 had an IC50 = 4.2 μg/ml against the HeLa cell line (cervical cancer) and binding energy against 5GWK (-8.32688 kcal/mol), 1PFK (-6.4780 kcal/mol) and 1TUP (-6.5279 kcal/mol) in the docking study. Conclusion: The obtained results reveal that these analogues exhibit potent antimicrobial and cytotoxic potential.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 23 vom: 20. Dez., Seite 2165-2179 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Islam, Shamsul [VerfasserIn] |
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| Links: |
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| Themen: |
220236ED28 |
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| Anmerkungen: |
Date Completed 20.12.2023 Date Revised 20.12.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0245 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM364737573 |
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| 520 | |a Aim: To synthesize and explore the therapeutic potential of amodiaquine analogues. Methodology: New promising analogues were synthesized by nucleophilic substitution at the 4-amino position and were characterized using 1H NMR, 13C NMR and FT-IR spectroscopic techniques. Results: Antibacterial and cytotoxic screening revealed the high potency of these compounds; analogue AS1 had an 34.3 ± 0.18 mm zone of inhibition against Pseudomonas aeruginosa. Excellent activity against fungal strains, that is, Candida albicans (39.6 ± 0.23 mm) was shown by analogue AS2. Analogue AS1 had an IC50 = 4.2 μg/ml against the HeLa cell line (cervical cancer) and binding energy against 5GWK (-8.32688 kcal/mol), 1PFK (-6.4780 kcal/mol) and 1TUP (-6.5279 kcal/mol) in the docking study. Conclusion: The obtained results reveal that these analogues exhibit potent antimicrobial and cytotoxic potential | ||
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