Compounds that suppress cancer cells and exhibit antitumor...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/26 (2006.01) A61K 31/196 (2006.01) A61K 31/451 (2006.01) A61P 35/00 (2006.01) C07C 311/19 (2006.01)

Patent

CA 2757912

The present invention provides compounds S31-201.1066 (Formula 1) and S31-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.

La présente invention concerne des composés S3I-201.1066 (Formule 1) et S3I-201.2096 (Formule 2) en tant qu'agents de liaison Stat3 sélectifs qui bloquent l'association de Stat3 avec les motifs pTyr du récepteur cognat, la phosphorylation de Stat3 et la translocation nucléaire, la fonction transcriptionnelle de Stat3, et par conséquent induisent des effets cellulaires antitumoraux spécifiques à Stat3 in vitro et une réponse antitumorale in vivo.

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