Design, synthesis and evaluation of novel 19F magnetic resonance sensitive protein tyrosine phosphatase inhibitors

Yu Li; Guiquan Xia; Qi Guo; Li Wu; Shizhen Chen; Zhigang Yang; Wei Wang; Zhong-Yin Zhang; Xin Zhou; Zhong-Xing Jiang

doi:10.1039/C6MD00277C

Design, synthesis and evaluation of novel ¹⁹F magnetic resonance sensitive protein tyrosine phosphatase inhibitors†‡

Yu Li,^a Guiquan Xia,^a Qi Guo,^a Li Wu,^b Shizhen Chen,^c Zhigang Yang,^a Wei Wang,^a Zhong-Yin Zhang,^b Xin Zhou^c and Zhong-Xing Jiang*^acde

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* Corresponding authors

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

^b Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, 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

^e State Key Laboratory for Modification of Chemical Fibers and Polymer Materials, Donghua University, Shanghai 201620, China

Abstract

Fluorine is a highly attractive element for both medicinal chemistry and imaging technologies. To facilitate protein tyrosine phosphatase (PTP)-targeted drug discovery and imaging-guided PTP research on fluorine, several highly potent and ¹⁹F MR sensitive PTP inhibitors were discovered through a structure-based focused library strategy.

MedChemComm

Design, synthesis and evaluation of novel ¹⁹F magnetic resonance sensitive protein tyrosine phosphatase inhibitors†‡

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Design, synthesis and evaluation of novel ¹⁹F magnetic resonance sensitive protein tyrosine phosphatase inhibitors

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