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

Stefania Grimaudo, Carlota Lopez Cara, Olga Cruz-Lopez, Nicola Zonta, Taradas Sarkar, Ernest Hamel, Mojgan Aghazadeh Tabrizi, Jan Balzarini, Andrea Brancale, Delia Preti, Maria Dora Carrion, Pier Giovanni Baraldi, Romeo Romagnoli, Hsing-Pang Hsieh, Antonietta Di Cristina

Risultato della ricerca: Articlepeer review

82 Citazioni (Scopus)

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.
Lingua originaleEnglish
pagine (da-a)1464-1468
RivistaJournal of Medicinal Chemistry
VolumeMar13;51(5)
Stato di pubblicazionePublished - 2008

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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