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- Title
Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest.
- Authors
Gabriele, Elena; Porta, Federica; Facchetti, Giorgio; Galli, Corinna; Gelain, Arianna; Meneghetti, Fiorella; Rimoldi, Isabella; Romeo, Sergio; Villa, Stefania; Ricci, Chiara; Ferri, Nicola; Akira Asai; Barlocco, Daniela; Sparatore, Anna
- Abstract
Here we report synthetic methodology affording in the most efficient way the rapid preparation of new dithiolethiones (DTTs) and methanethiosulfonates (MTSs). These were evaluated as STAT3 inhibitors since these electrophilic systems could react with thiol groups of STAT3-SH2 domain. The results showed that MTSs strongly interacted with the SH2 domain, whereas the corresponding DTTs possessed lower affinity, independently from the nature of the linked heterocyclic scaffold.
- Subjects
THIONES; SULFONATES; METHANE synthesis; ELECTROPHILIC addition reactions; CHEMICAL affinity; COUPLING reactions (Chemistry)
- Publication
ARKIVOC: Online Journal of Organic Chemistry, 2017, Vol 2017, p235
- ISSN
1551-7004
- Publication type
Article
- DOI
10.3998/ark.5550190.p009.805