Bioorganic and Medicinal Chemistry Letters p. 2957 - 2960 (2018)
Update date:2022-08-03
Topics:
Huang, Yaping
Sun, Geng
Wang, Pengfei
Shi, Rui
Zhang, Yanchun
Wen, Xiaoan
Sun, Hongbin
Chen, Caiping
In this study, Complex I inhibitor R419 was firstly revealed to have significant anticancer activity against HepG2 cells (IC50 = 5.2 ± 0.9 μM). Based on this finding, a series of R419 derivatives were synthesized and biologically evaluated. As results, 9 derivatives were found to have obvious anticancer activity. Among them, H20 exhibited the most potent activity (IC50 = 2.8 ± 0.4 μM). Mechanism study revealed that H20 caused severe depletion of cellular ATP, dose-dependently activated AMPK, decreased Bcl-2/Bax ratio and induced necrotic cell death. Most importantly, H20 displayed definite inhibitory activity against Complex I.
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