期刊
MOLECULES
卷 23, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/molecules23092126
关键词
ferrocene; anticancer; MNK; cell viability; spheroids
资金
- Biotechnology and Biological Sciences Research Council (UK) [BB/L018209/1]
- EPSRC [EP/P026990/1]
- Thai Royal Government
- School of Life Sciences, University of Sussex
- BBSRC [BB/L018209/1] Funding Source: UKRI
Two novel ferrocene-containing compounds based upon a known MNK1/2 kinase (MAPK-interacting kinase) inhibitor have been synthesized. The compounds were designed to use the unique shape of ferrocene to exploit a large hydrophobic pocket in MNK1/2 that is only partially occupied by the original compound. Screening of the ferrocene analogues showed that both exhibited potent anticancer effects in several breast cancer and AML (acute myeloid leukemia) cell lines, despite a loss of MNK potency. The most potent ferrocene-based compound 5 was further analysed in vitro in MDA-MB-231 (triple negative breast cancer cells). Dose-response curves of compound 5 for 2D assay and 3D assay generated IC50 values (half maximal inhibitory concentration) of 0.55 mu M and 1.25 mu M, respectively.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据