A series of ester and amide derivatives of triterpenoid saponin saponin D (PSD) were designed, synthesized, and evaluated for their antiproliferative activity. Compounds 1 and 6 displayed 1.7-8.3 times more potent cytotoxicity (IC = 1.2-4.7 and 1.7-4.5 μM, respectively) against five human tumor cell lines (SMMC-7721, MCF-7, NCI-H460, A549, and HCT-116) and lower acute toxicity to mice than did PSD. Furthermore, compound 6 was observed to show potent tumor growth inhibition against mice H22 hepatocellular cells (49.8% at 20 mg/kg) and induce cell cycle at G phase and apoptosis in HCT-116 cells.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6804646 | PMC |
| http://dx.doi.org/10.3389/fphar.2019.01208 | DOI Listing |
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