Academic Journal
A trimethyl lock successfully stabilizes a nascent Michael acceptor for prodrug applications.
| Τίτλος: | A trimethyl lock successfully stabilizes a nascent Michael acceptor for prodrug applications. |
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| Συγγραφείς: | Cheema EK; Department of Chemistry, Johns Hopkins University, Baltimore, MD 21218, USA. rokita@jhu.edu., Rokita SE; Department of Chemistry, Johns Hopkins University, Baltimore, MD 21218, USA. rokita@jhu.edu. |
| Πηγή: | Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2026 Oct 15; Vol. 62 (81), pp. 20326-20329. Date of Electronic Publication: 2026 Oct 15. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 9610838 Publication Model: Electronic Cited Medium: Internet ISSN: 1364-548X (Electronic) Linking ISSN: 13597345 NLM ISO Abbreviation: Chem Commun (Camb) Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Cambridge : Royal Society of Chemistry |
| Ιατρικοί όροι (MeSH): | Prodrugs*/chemistry , Prodrugs*/pharmacology , Prodrugs*/metabolism , STAT3 Transcription Factor*/antagonists & inhibitors , STAT3 Transcription Factor*/metabolism , Pyrones*/chemistry , Pyrones*/pharmacology, NAD(P)H Dehydrogenase (Quinone)/metabolism ; Humans |
| Περίληψη: | 5-Hydroxy-γ-pyrone-based Michael acceptors have repeatedly registered as hits in screens for inhibiting key therapeutic targets, but their aqueous instability has prevented further development. Here, we report a method to stabilize such an inhibitor of STAT3 with a trimethyl lock until reduction by hNQO1, an enzyme typically overexpressed in hypoxic tumors. |
| Substance Nomenclature: | 0 (Prodrugs) 0 (STAT3 Transcription Factor) EC 1.6.5.2 (NAD(P)H Dehydrogenase (Quinone)) 0 (Pyrones) |
| Entry Date(s): | Date Created: 20260921 Date Completed: 20261015 Latest Revision: 20261015 |
| Update Code: | 20261016 |
| DOI: | 10.1039/d6cc05508g |
| PMID: | 42766013 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1364-548X |
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| DOI: | 10.1039/d6cc05508g |