Bioorganic and Medicinal Chemistry Letters p. 7530 - 7533 (2012)
Update date:2022-08-02
Topics:
Liu, Yingqian
Qian, Keduo
Wang, Chih-Ya
Chen, Chin-Ho
Yang, Xiaoming
Lee, Kuo-Hsiung
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.
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