Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest
Articolo
Data di Pubblicazione:
2017
Citazione:
Synthesis of new dithiolethione and methanethiosulfonate systems endowed
with pharmaceutical interest / E. Gabriele, F. Porta, G. Facchetti, C. Galli, A. Gelain, F. Meneghetti, I. Rimoldi, S. Romeo, S. Villa, C. Ricci, N. Ferri, A. Asai, D. Barlocco, A. Sparatore. - In: ARKIVOC. - ISSN 1551-7012. - 2017:ii(2017), pp. 235-250. [10.3998/ark.5550190.p009.805]
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.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
1,2,5-Oxadiazole; N-Methylimidazole; STAT3-SH2 domain; Coupling reactions
Elenco autori:
E. Gabriele, F. Porta, G. Facchetti, C. Galli, A. Gelain, F. Meneghetti, I. Rimoldi, S. Romeo, S. Villa, C. Ricci, N. Ferri, A. Asai, D. Barlocco, A. Sparatore
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