A library of 1,2,3-triazole-substituted oleanolic acid derivatives as anticancer agents: design, synthesis, and biological evaluationElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ob01605j
A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu( i ) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. The anti-proliferative evaluation indicated that some compounds exhibited excellent anti-cancer activity against the exa...
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Sprache: | eng |
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Zusammenfassung: | A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu(
i
) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. The anti-proliferative evaluation indicated that some compounds exhibited excellent anti-cancer activity against the examined cancer cell lines. Among all derivatives, compound
3t
possesses the best inhibitory activity against HT1080 cells. A series of pharmacology experiments show that compound
3t
significantly induced HT1080 cell apoptosis. Therefore, this compound can serve as a promising lead candidate for further study.
A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu(
i
) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. |
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ISSN: | 1477-0520 1477-0539 |
DOI: | 10.1039/c4ob01605j |