药效团
K562细胞
白血病
一氧化氮
化学
髓系白血病
药理学
体外
榄香烯
化疗
癌症研究
生物化学
医学
免疫学
细胞凋亡
内科学
有机化学
作者
Junlong Zhu,Xiaoying Jiang,Xinyu Luo,Rui Zhao,Junjie Li,Hong Cai,Xiang‐Yang Ye,Renren Bai,Tian Xie
摘要
Abstract This study aimed to design and synthesize active hybrids of β ‐elemene and nitric oxide (NO) donor pharmacophore as potential agents for treating leukemia. Derivatives reported herein exerted better inhibitory effects against human chronic myeloid leukemia K562 cells compared to β ‐elemene (IC 50 > 100 μM). The most potent compound 18f showed an IC 50 value of 0.53 μM against K562 cells, as well as a high NO release level in vitro. In the K562 xenograft tumor mice model, compound 18f effectively inhibited the growth of the tumor, with a significant inhibition rate of 73.18%. After treatment with compound 18f , the body weight of mice did not decrease, indicating that it possessed good safety profile. All these proved that compound 18f was an excellent potential agent against leukemia.
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