STAT3 Inhibitory Activity of Structurally Simplified Withaferin A Analogues.

Tahara, Teruyuki; Streit, Ursula; Pelish, Henry E; Shair, Matthew D

Tahara, Teruyuki; Streit, Ursula; Pelish, Henry E; Shair, Matthew D.

Afiliación

Tahara T; Department of Chemistry and Chemical Biology, Harvard University , 12 Oxford Street, Cambridge, Massachusetts 02138, United States.
Streit U; Department of Chemistry and Chemical Biology, Harvard University , 12 Oxford Street, Cambridge, Massachusetts 02138, United States.
Pelish HE; Department of Chemistry and Chemical Biology, Harvard University , 12 Oxford Street, Cambridge, Massachusetts 02138, United States.
Shair MD; Department of Chemistry and Chemical Biology, Harvard University , 12 Oxford Street, Cambridge, Massachusetts 02138, United States.

Org Lett ; 19(7): 1538-1541, 2017 04 07.

Article en En | MEDLINE | ID: mdl-28350459

RESUMEN

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.

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: Org Lett Asunto de la revista: BIOQUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos

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