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Article

Expanding the Chemistry of Dihaloacetamides as Tunable Electrophiles for Reversible Covalent Targeting of Cysteines.

Journal of medicinal chemistry - 13 Jul 2023

Yamane Daiki, Tetsukawa Ryo, Zenmyo Naoki, Tabata Kaori, Yoshida Yuya, Matsunaga Naoya, Shindo Naoya, Ojida Akio

Abstract excerpt

The choice of an appropriate electrophile is crucial in the design of targeted covalent inhibitors (TCIs). In this report, we systematically investigated the glutathione (GSH) reactivity of various haloacetamides and the aqueous stability of their thiol adducts. Our findings revealed that dihaloacetamides cover a broad range of GSH reactivity depending on the combination of the halogen atoms and the structure of...

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PMID: 37393576
DOI: 10.1021/acs.jmedchem.3c00737

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