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.
New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors / E. Gabriele, D. Brambilla, C. Ricci, L. Regazzoni, K. Taguchi, N. Ferri, A. Asai, A. Sparatore. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - 32:1(2017 Dec), pp. 1012-1028.
|Titolo:||New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors|
GABRIELE, ELENA (Primo)
SPARATORE, ANNA CONCETTINA (Ultimo)
|Parole Chiave:||anticancer drug; NF-κB inhibitors; STAT3 inhibitors; cytotoxicity; methanethiosulfonate derivatives|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
Settore BIO/14 - Farmacologia
|Data di pubblicazione:||dic-2017|
|Data ahead of print / Data di stampa:||lug-2017|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1080/14756366.2017.1350658|
|Appare nelle tipologie:||01 - Articolo su periodico|