STAT3 Inhibitory Activity of Structurally Simplified Withaferin A Analogues

Signal transducer and activator of transcription 3 (STAT3) is a component of the JAK/STAT pathway. Therapeutic inhibition of STAT3 has been of high interest, as its aberrant activation has been linked to cancer, inflammation, and other human diseases. The withanolide family natural product withaferi...

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Bibliographic Details
Published in:Organic letters 2017-04, Vol.19 (7), p.1538-1541
Main Authors: Tahara, Teruyuki, Streit, Ursula, Pelish, Henry E, Shair, Matthew D
Format: Article
Language:English
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Summary:Signal transducer and activator of transcription 3 (STAT3) is a component of the JAK/STAT pathway. Therapeutic inhibition of STAT3 has been of high interest, as its aberrant activation has been linked to cancer, inflammation, and other human diseases. The withanolide family natural product withaferin A (1) inhibits STAT3 activation. We designed, synthesized, and evaluated simplified withanolide analogues SLW1 (3) and SLW2 (4), and found that SLW1 retained the STAT3 inhibitory activity of withaferin A.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.7b00332