Synthesis and evaluation of anticancer activity of quillaic acid derivatives: A cell cycle arrest and apoptosis inducer through NF-κB and MAPK pathways

A series of quillaic acid derivatives with different substituents on the 28-carboxyl group were designed and synthesized. Five human cancer cell lines (HCT116, BEL7402, HepG2, SW620, and MCF-7) were evaluated for their antitumor activity in vitro. Some of the tested derivatives showed improved antiproliferative activity compared to the lead compound, quillaic acid. Among them, compound E (IC50 = 2.46 +/- 0.44 mu M) showed the strongest antiproliferative activity against HCT116 cells; compared with quillaic acid (IC50 > 10 mu M), its efficacy against HCT116 cancer cells was approximately 4-fold higher than that of quillaic acid. Compound E also induces cell cycle arrest and apoptosis by modulating NF-kappa B and MAPK pathways. Therefore, the development of compound E is certainly valuable for anti-tumor applications.

Automated summary

A series of quillaic acid derivatives with different substituents were synthesized and evaluated for their antitumor activity against human cancer cell lines. One compound showed strong antiproliferative activity and induced apoptosis and cell cycle arrest by modulating signaling pathways.