New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors. (1st January 2017)

• Record Type: Journal Article
• Authors: Gabriele, Elena; Brambilla, Dario; Ricci, Chiara; Regazzoni, Luca; Taguchi, Kyoko; Ferri, Nicola; Asai, Akira; Sparatore, Anna
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 32:Number 1(2017)
• Page Start: 1012
• Page End: 1028
• Publication Date: 2017-01-01
• Subjects: Anticancer drug -- cytotoxicity -- STAT3 inhibitors -- NF-κB inhibitors -- methanethiosulfonate derivatives; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2017.1350658
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most of the new hybrid compounds were able to strongly and selectively bind to STAT3, whereas the parent drugs were devoid of this ability at the tested concentrations. Some of them were also able to inhibit the NF-κB transcriptional activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro with IC50 in micromolar range, thus suggesting a potential anticancer activity. Taken together, our study described the identification of new derivatives with dual STAT3/NF-κB inhibitory activity, which may represent hit compounds for developing multi-target anticancer agents. Graphical Abstract: