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Design, synthesis and antiproliferative activity in cancer cells of novel 18β-glycyrrhetinic acid derivatives

Huang, M.; Li, K.; Jin, S.-y.; Cui, T.-x.; Liu, D.; Zhao, L.-x.

Yao Xue Xue Bao 50(10): 1263-1271

2015

ISSN/ISBN: 0513-4870
PMID: 26837172
Document Number: 682625
To investigate the anticancer effects of ring C in 18β-glycyrrhetinic acid (GA), a series of GA derivatives featured with 9(11)-ene moiety in ring C were designed and synthesized. The structures were confirmed by IR, LC-MS and 1H NMR. Their inhibitory effects towards human prostate cancer PC-3 and leukemia HL-60 cell lines were determined. Most of the derivatives displayed stronger antiproliferative activities than GA. Particularly, compound 14 showed promising anticancer activity with the GI50 values of 4.48 µmol · L(-1) and 1.2 µmol · L(-1) against PC-3 and HL-60 cells respectively, which is worth further study.

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