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.
View MoreShanghai WinTide BioTechnology Co.,Ltd
Contact:86-21-37100630
Address:No. 908 Yunhe Road, Fengxian district, Shanghai
Jinhua City Mingzhu Pharmaceutical Co.,Ltd.
Contact:15857995878 0579-82207761
Address:No.169 Shenze Road, New Area,Jinpan Development Zone, Jinhua
Jinzhou Jiutai Pharmaceutical Co.,Ltd
Contact:+86-0416-5179890
Address:No.41, Taianli, Taihe District, Jinzhou, Liaoning
Feiyang Biotechnology Co., Ltd.
Contact:+86-533-7866339
Address:Qilu Chemistry Park, 200m north of Management Community Building of Park
Hubei Xiangxi Chemical Industry Co.,Ltd
Contact:+86-710-3454830
Address:No.7, Daqing East Road, Xiangfan City, Hubei Province, China
Doi:10.1002/ardp.19753080310
(1975)Doi:10.1021/acs.orglett.1c01813
(2021)Doi:10.1021/jo00069a035
(1993)Doi:10.1002/jlcr.2580120214
(1976)Doi:10.1002/bms.1200060305
(1979)Doi:10.1016/S0957-4166(03)00160-5
(2003)