NWIPB OpenIR
Discovery of antitumor ursolic acid long-chain diamine derivatives as potent inhibitors of NF-kappa B
Jiang, Wei; Huang, Ri-Zhen; Zhang, Jing; Guo, Tong; Zhang, Meng-Ting; Huang, Xiao-Chao; Zhang, Bin; Liao, Zhi-Xin; Sun, Jing; Wang, Heng-Shan
2018
Source PublicationBIOORGANIC CHEMISTRY
Volume79
AbstractA series of inhibitors of NF-kappa B based on ursolic acid (UA) derivatives containing long-chain diamine moieties were designed and synthesized as well as evaluated the antitumor effects. These compounds exhibited significant inhibitory activity to the NF-kappa B with IC50 values at micromolar concentrations in A549 lung cancer cell line. Among them, compound 8c exerted potent activity against the test tumor cell lines including multidrug resistant human cancer lines, with the IC50 values ranged from 5.22 to 8.95 mu M. Moreover, compound 8c successfully suppressed the migration of A549 cells. Related mechanism study indicated compound 8c caused cell cycle arrest at G1 phase and triggered apoptosis in A549 cells through blockage of NF-kappa B signalling pathway. Molecular docking study revealed that key interactions between 8c and the active site of NF-kappa B in which the bulky and strongly electrophilic group of long-chain diamine moieties were important for improving activity.
KeywordUrsolic acid Long-chain diamine NF-kappa B Drug resistance Migration
Document Type期刊论文
Identifierhttp://210.75.249.4/handle/363003/59990
Collection中国科学院西北高原生物研究所
Recommended Citation
GB/T 7714
Jiang, Wei,Huang, Ri-Zhen,Zhang, Jing,et al. Discovery of antitumor ursolic acid long-chain diamine derivatives as potent inhibitors of NF-kappa B[J]. BIOORGANIC CHEMISTRY,2018,79.
APA Jiang, Wei.,Huang, Ri-Zhen.,Zhang, Jing.,Guo, Tong.,Zhang, Meng-Ting.,...&Wang, Heng-Shan.(2018).Discovery of antitumor ursolic acid long-chain diamine derivatives as potent inhibitors of NF-kappa B.BIOORGANIC CHEMISTRY,79.
MLA Jiang, Wei,et al."Discovery of antitumor ursolic acid long-chain diamine derivatives as potent inhibitors of NF-kappa B".BIOORGANIC CHEMISTRY 79(2018).
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