With the aim to discover new STAT3 direct inhibitors, potentially useful as anticancer agents, a set of methanethiosulfonate drug hybrids were synthesized. The in vitro tests showed that all the thiosulfonic compounds were able to strongly and selectively bind STAT3-SH2 domain, whereas the parent drugs were completely devoid of this ability. In addition, some of them showed a moderate antiproliferative activity on HCT-116 cancer cell line. These results suggest that methanethiosulfonate moiety can be considered a useful scaffold in the preparation of new direct STAT3 inhibitors. Interestingly, an unusual kind of organosulfur derivative, endowed with valuable antiproliferative activity, was occasionally isolated.
Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain / E. Gabriele, C. Ricci, F. Meneghetti, N. Ferri, A. Asai, A. Sparatore. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - 32:1(2017), pp. 337-344.
|Titolo:||Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain|
GABRIELE, ELENA (Primo)
RICCI, CHIARA (Secondo)
SPARATORE, ANNA CONCETTINA (Corresponding)
|Parole Chiave:||anticancer drug; cytotoxicity; SH2 antagonist; STAT3; S3I-201 analogs|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
Settore BIO/14 - Farmacologia
|Data di pubblicazione:||2017|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1080/14756366.2016.1252757|
|Appare nelle tipologie:||01 - Articolo su periodico|