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Updated: Jun 27, 2026

Co-immunoprecipitation Assay Using Endogenous Nuclear Proteins from Cells Cultured Under Hypoxic Conditions
Published on: August 2, 2018
Switchable Reactivity of Hydrazonoyl Halides: Enabling the Discovery of Potent Hypoxia-Inducible Factor Inhibitors
Xiaochen Tian1,2,3, Hongli Wu4, Yaoyu Shi1
1Molecular Synthesis Center & Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao 266003, China.
Abstract:
A substituent-regulated divergent cycloaddition reaction between hydrazonoyl halides and 2-aminochalcones has been developed. In this study, substituents effectively reversed the intrinsic reactivity of hydrazonoyl halides, marking the first instance where hydrazonoyl halides can function as C1 synthonswith the azomethine carbon displaying unprecedented nucleophilic reactivity, a property that deviates from the established paradigms of hydrazonoyl halide chemistry. The reaction mechanism underlying this methodology was verified via density functional theory calculations. Moreover, biological activity evaluations demonstrated that the synthesized indolines suppress hypoxia-inducible factor activity both in vitro and in vivo, indicating that these compounds are promising candidates for further development as potential anticancer agents.
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