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Identification of galiellalactone-based novel STAT3-selective inhibitors with cytotoxic activities against triple-negative breast cancer cell lines
Cited 17 time in
Web of Science
Cited 15 time in Scopus
- Authors
- Issue Date
- 2017-10
- Publisher
- Pergamon Press Ltd.
- Citation
- Bioorganic and Medicinal Chemistry, Vol.25 No.19, pp.5032-5040
- Abstract
- Signal transducer and activator of transcription 3 (STAT3) is phosphorylated in breast cancer cells, particularly triple-negative breast cancers (TNBCs). Therefore, the inhibition of constitutive phosphorylated STAT3 is a promising therapeutic for TNBC treatment. Recently, a series of novel STAT3 inhibitors based on natural (-)-galiellalactone have been identified to inhibit STAT3 phosphorylation at the Tyr705 residue. Interestingly, the truncation of the cyclohexene moiety of (-)-galiellalactone to [3.3] bicyclic lactone as a pharmacophoric core produced improved cytotoxic effects against TNBCs. The potent analogues 16 and 17, identified from a STAT3-mediated luciferase reporter assay, selectively inhibited the STAT3 signaling pathway without affecting STAT1 or STAT5. (C) 2017 Elsevier Ltd. All rights reserved.
- ISSN
- 0968-0896
- Language
- English
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