Design, synthesis and antiproliferative activity in cancer cells of novel 18β-glycyrrhetinic acid derivatives.
- Author:
Min HUANG
;
Kun LI
;
Shu-yu JIN
;
Ting-xiu CUI
;
Dan LIU
;
Lin-xiang ZHAO
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemistry;
pharmacology;
Cell Line, Tumor;
drug effects;
Cell Proliferation;
drug effects;
Drug Design;
Glycyrrhetinic Acid;
analogs & derivatives;
chemistry;
HL-60 Cells;
drug effects;
Humans;
Male;
Prostatic Neoplasms;
pathology
- From:
Acta Pharmaceutica Sinica
2015;50(10):1263-1271
- 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.
