Monday, January 15, 2024

Diazepam-based covalent modifiers of GPX4 induce ferroptosis in liver cancer cells

D. Yadav, S. Tiwari, S. Senthil, S. K. Vechalapu, S. Duraisamy, V. Rawat, M. I. Rahman, S. Khanna and D. Allimuthu, 

Chem. Commun., 2024

DOI: 10.1039/D3CC06215E

Developing new chemotherapeutics that are structurally and mechanistically unique is a need due to the rapid rise of cancer incidences across the globe. Here we report the identification of irreversible, thiol-reactive diazepam derivatives as GPX4 modifiers and nanomolar inducers of ferroptosis in liver cancer cells.



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N-Acyl-N-alkyl/aryl Sulfonamide Chemistry Assisted by Proximity for Modification and Covalent Inhibition of Endogenous Proteins in Living Systems

Tomonori Tamura and Itaru Hamachi Accounts of Chemical Research 2025 58 (1), 87-100 DOI: 10.1021/acs.accounts.4c00628 Selective chemical mo...