Synthesis and evaluation of new Hsp90 inhibitors based on a 1, 4, 5-trisubstituted 1, 2, 3-triazole scaffold

M Taddei, S Ferrini, L Giannotti, M Corsi…

Index: Taddei, Maurizio; Ferrini, Serena; Giannotti, Luca; Corsi, Massimo; Manetti, Fabrizio; Giannini, Giuseppe; Vesci, Loredana; Milazzo, Ferdinando M.; Alloatti, Domenico; Guglielmi, Mario B.; Castorina, Massimo; Cervoni, Maria L.; Barbarino, Marcella; Fodera, Rosanna; Carollo, Valeria; Pisano, Claudio; Armaroli, Silvia; Cabri, Walter Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2258 - 2274

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Citation Number: 19

Abstract

Ruthenium catalyzed 1, 3-cycloaddition (click chemistry) of an azido moiety installed on dihydroxycumene scaffold with differently substituted aryl propiolates gave a new family of 1, 4, 5-trisubstituted triazole carboxylic acid derivatives that showed high affinity toward Hsp90 associated with cell proliferation inhibition, both in nanomolar range. The 1, 5 arrangement of the resorcinol, the aryl moieties, and the presence of an alkyl (secondary) amide in ...