Asymmetrically Substituted m ‐Terphenyl Phosphates Inhibit the Transcription Factor STAT5a
Abstract: We recently presented Stafia‐1 as the first chemical entity that inhibits the transcription factor STAT5a with selectivity over the highly homologous STAT5b. Stafia‐1, which was identified from a series of symmetrically substituted m‐terphenyl phosphates, binds to the interface between the SH2 domain and the linker domain of STAT5a. Here, we outline a synthetic strategy for the synthesis of asymmetrically substituted m‐terphenyl phosphates, which can be tailored to address their asymmetric STAT5a binding site in a more specific manner. The asymmetrically substituted m‐terphenyl phosphate with the highest activity against STAT5a was converted to a phosphatase‐stable monofluoromethylene phosphonate. The synthetic methodology and activity analysis described here provide first insights into the structure‐activity relationships of m‐terphenyl phosphates for use as selective STAT5a inhibitors.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Asymmetrically Substituted m ‐Terphenyl Phosphates Inhibit the Transcription Factor STAT5a ; day:29 ; month:12 ; year:2021 ; extent:1
ChemBioChem ; (29.12.2021) (gesamt 1)
- Creator
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Müller‐Klieser, Daniel
Berg, Thorsten
- DOI
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10.1002/cbic.202100603
- URN
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urn:nbn:de:101:1-2021123014121734136932
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:36 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Müller‐Klieser, Daniel
- Berg, Thorsten
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