55874-07-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel spin labeled 18β-glycyrrhetinic acid derivatives
Liu, Yingqian,Qian, Keduo,Wang, Chih-Ya,Chen, Chin-Ho,Yang, Xiaoming,Lee, Kuo-Hsiung
, p. 7530 - 7533 (2012)
Eighteen novel spin-labeled 18β-glycyrrhetinic acid (GA) derivatives were designed, synthesized, and evaluated for cytotoxicity against four human tumor cell lines (A-549, DU-145, KB and KBvin). Most of the derivatives showed more significant cytotoxicity than that of the parent compound GA. The best compound, 6j, with a tryptophan amino moiety and piperidine nitroxyl radical showed GI50 values of 13.7-15.0 μM, and was fivefold more potent than GA. In a mechanism of action study, compound 7a was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings support further optimization efforts based on 18β-GA as a lead compound to develop potential anticancer drug candidates.
