Discovery of a 19F MRI sensitive salinomycin derivative with high cytotoxicity towards cancer cells

Qiuyan Shi; Yu Li; Shaowei Bo; Xiaofei Li; Peng Zhao; Qi Liu; Zhigang Yang; Hengjiang Cong; Hexiang Deng; Mingnan Chen; Shizhen Chen; Xin Zhou; Hong Ding; Zhong-Xing Jiang

doi:10.1039/C6CC01508E

Discovery of a ¹⁹F MRI sensitive salinomycin derivative with high cytotoxicity towards cancer cells†

Qiuyan Shi,^a Yu Li,^a Shaowei Bo,^a Xiaofei Li,^a Peng Zhao,^b Qi Liu,^a Zhigang Yang,^a Hengjiang Cong,^a Hexiang Deng,^a Mingnan Chen,^b Shizhen Chen,^c Xin Zhou,^c Hong Ding^a and Zhong-Xing Jiang*^ad

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* Corresponding authors

^a School of Pharmaceutical Sciences and College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430071, China
E-mail: zxjiang@whu.edu.cn

^b Department of Pharmaceutics and Pharmaceutical Chemistry, School of Pharmacy, University of Utah, Salt Lake City, Utah 84112, USA

^c State Key Laboratory for Magnetic Resonance and Atomic and Molecular Physics, Wuhan Institute of Physics and Mathematics, Chinese Academy of Sciences, Wuhan 430071, China

^d Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China

Abstract

Salinomycin is a promising anti-cancer agent which selectively targets cancer stem cells. To improve its potency and selectivity, an analog library of salinomycin was generated by site-specific modification and CuAAc derivatization. Through a cytotoxicity analysis of the library, a fluorinated analog with high potency, selectivity, and ¹⁹F MRI sensitivity was discovered as a novel theranostic agent.

Chemical Communications

Discovery of a ¹⁹F MRI sensitive salinomycin derivative with high cytotoxicity towards cancer cells†

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Discovery of a ¹⁹F MRI sensitive salinomycin derivative with high cytotoxicity towards cancer cells

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