Design, synthesis and antiproliferative activity in cancer cells of novel 18β-glycyrrhetinic acid derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 1263-1271, 2015.
Article
in Zh
| WPRIM
| ID: wpr-320091
Responsible library:
WPRO
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.
Full text:
1
Database:
WPRIM
Main subject:
Pathology
/
Pharmacology
/
Prostatic Neoplasms
/
Drug Design
/
Chemistry
/
HL-60 Cells
/
Cell Line, Tumor
/
Cell Proliferation
/
Glycyrrhetinic Acid
/
Antineoplastic Agents
Limits:
Humans
/
Male
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2015
Document type:
Article