Journal
MOLECULES
Volume 22, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/molecules22111876
Keywords
betulin; 1,3-dipolar cycloaddition; triazoles; antiviral activity; anticancer activity; antimicrobial activity
Funding
- Medical University of Silesia in Katowice, Poland [KNW-1-015/K/7/O, KNW-2-011/N/7/N]
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Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by H-1 and C-13 NMR, IR, and high-resolution mass spectrometry (HR-MS) analysis. The target triazoles were screened for their antiviral activity against DNA and RNA viruses. The cytotoxic activity of the obtained compounds 5a-k and 6a-h was determined using five human cancer cell lines (T47D, MCF-7, SNB-19, Colo-829, and C-32) by a WST-1 assay. The bistriazole 6b displayed a promising IC50 value (0.05 M) against the human ductal carcinoma T47D (500-fold higher potency than cisplatin). The microdilution method was applied for an evaluation of the antimicrobial activity of all of the compounds. The triazole 5e containing a 3-deoxythymidine-5-yl moiety exhibited antibacterial activity against two gram-negative bacteria vz. Klebsiella pneumoniae and Escherichia coli (minimal inhibitory concentration (MIC) range of 0.95-1.95 M).
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