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.
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]
Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest
E. GabrielePrimo
;F. PortaSecondo
;G. Facchetti;C. Galli;A. Gelain;F. Meneghetti;I. Rimoldi;S. Romeo;S. Villa;C. Ricci;D. BarloccoPenultimo
;A. Sparatore
2017
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.File | Dimensione | Formato | |
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