Design, synthesis and antiproliferative activity in cancer cells of novel 18β-glycyrrhetinic acid derivatives.
- Author:
Min HUANG
;
Kun LI
;
Shuyu JIN
;
Tingxiu CUI
;
Dan LIU
;
Linxiang ZHAO
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2015;50(10):1263-71
- CountryChina
- Language:Chinese
-
Abstract:
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.
