Targeting the Grb2 cSH3 domain: Design, synthesis and biological evaluation of the first series of modulators

Marianna Bufano,Michela Puxeddu,Marianna Nalli,Giuseppe La Regina,Angelo Toto,Francesca Romana Liberati,Alessio Paone,Francesca Cutruzzolà,Domiziana Masci,Chiara Bigogno,Giulio Dondio,Romano Silvestri,Stefano Gianni,Antonio Coluccia

Bioorganic Chemistry（2023）

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摘要

•The derivatives proven to be inhibitors of Grb2 targeting the cSH3 domain.•Five derivatives showed antitumoral activity in the range of one-digit μM concentration.•Derivatives 12 had a one-digit μM concentration inhibition against H1299, SKOV3 and U87 cell lines.

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关键词

Grb2-Gab2 system, SH3 domain, Anticancer, Small Molecules, Structure activity Relationship

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