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STEFANIA GRIMAUDO

Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors

  • Authors: ROMAGNOLI R; BARALDI PG; SARKAR T; CARRION MD; CARA CL; CRUZ-LOPEZ O; PRETI D; TABRIZI MA; TOLOMEO M; GRIMAUDO S; DI CRISTINA A; ZONTA N; BALZARINI J; BRANCALE A; HSIEH HP; HAMEL E
  • Publication year: 2008
  • Type: Articolo in rivista
  • OA Link: http://hdl.handle.net/10447/34018

Abstract

The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.