Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues

Shamsul Islam, Sohail A. Shahzad,Tariq Ismail, Usman A. S. Sherani, Kashif M. Khan, Nighat Fatima, Shujaat A. Khan,Abdul Mannan

FUTURE MEDICINAL CHEMISTRY(2024)

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摘要
Aim: To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential. Methods: Novel analogues were synthesized from chloroquine by nucleophilic substitution reaction at the 4-amino position. Results: Analogue CS1 showed maximum antimicrobial potential (30.3 +/- 0.15 mm zone) against Pseudomonas aeruginosa and produced a 19.2 +/- 0.21 mm zone against Candida albicans, while CS0 produced no zone at the same concentration. Analogue CS9 has excellent cytotoxic potential (HeLa cell line), showing 100% inhibition (IC50 = 8.9 +/- 1.2 mu g/ml), compared with CS0 (61.9% inhibition at 30 mu g/ml). Conclusion: These synthesized chloroquine analogues have excellent activity against different microbial strains and cervical cancer cell lines (HeLa) compared with their parent molecule.
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关键词
cervical cancer,chloroquine,cytotoxic assay,quinoline,sulfonamides
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