Synthesis and biological evaluation of 20-epi-amino-20-deoxysalinomycin derivatives

Eur J Med Chem. 2018 Mar 25:148:279-290. doi: 10.1016/j.ejmech.2018.02.004.

Yu Li ¹, Qiuyan Shi ¹, Jiajia Shao ², Yaping Yuan ³, Zhigang Yang ¹, Shizhen Chen ³, Xin Zhou ³, Shijun Wen ², Zhong-Xing Jiang ⁴

Affiliations

1 Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China.
2 State Key Laboratory of Oncology in South China, Sun-Yat-sen University Cancer Center, Sun-Yat-sen University, Guangzhou, 510060, China.
3 State Key Laboratory for Magnetic Resonance and Atomic and Molecular Physics, Wuhan Institute of Physics and Mathematics, Chinese Academy of Sciences, Wuhan, 430071, China.
4 Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. Electronic address: zxjiang@whu.edu.cn.

PMID: 29466777 DOI: 10.1016/j.ejmech.2018.02.004

Abstract

To improve the druggability of salinomycin, a 20-epi-amino-20-deoxysalinomycin derivatives library was synthesized with high efficacy from which a few salinomycin derivatives with high potency and selectivity were identified through comprehensive cytotoxicity assay, including a fluorine-19 magnetic resonance sensitive tool molecule. Using a K-Ras cellular model, salinomycin and its derivatives showed different molecular mode of action from literature reports. These results would be valuable for developing salinomycin-based Cancer therapy.

Keywords

(19)F MRI; Anti-cancer drugs; K-ras pathway; Nature product modification; Salinomycin; Staudinger reaction.

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