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

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

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2024-02, Vol.6 (14), p.1928-1931
Main Authors: Yadav, Dharmendra K, Tiwari, Sona, Senthil, Sathyapriya, Vechalapu, Sai Kumari, Duraisamy, Santhosh, Rawat, Viral, Rahman, Mohammed Isfahur, Khanna, Shweta, Allimuthu, Dharmaraja
Format: Article
Language:English
Subjects:
Benzodiazepines
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Summary:Developing new chemotherapeutics that are structurally and mechanistically unique is needed due to the rapid rise of the cancer incidence 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. The rapid rise of multidrug resistance in cancer demands the development of structurally and mechanistically unique drugs candidates. We report targeted covalent GPX4 modifiers as nanomolar inducers of ferroptosis in liver cancer cells.
ISSN:1359-7345
1364-548X
DOI:10.1039/d3cc06215e