Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain.

Elena Gabriele, Chiara Ricci, Fiorella Meneghetti, Nicola Ferri, Akira Asai, Anna Sparatore

Journal of enzyme inhibition and medicinal chemistry 2017 Jan 18

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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 organo-sulfur derivative, endowed with valuable antiproliferative activity, was occasionally isolated. [Formula: see text].

Citation

Elena Gabriele, Chiara Ricci, Fiorella Meneghetti, Nicola Ferri, Akira Asai, Anna Sparatore. Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain. Journal of enzyme inhibition and medicinal chemistry. 2017 Jan 18;32(1):337-344