Synthesis and Biological Evaluation of 2- and 3-Aminobenzo[b]thiophene Derivatives as Antimitotic Agents and Inhibitors of Tubulin Polymerization.

Stefania Grimaudo, Carlota Lopez Cara, Ernest Hamel, Mojgan Aghazadeh Tabrizi, Jan Balzarini, Francesca Fruttarolo, Andrea Brancale, Delia Preti, Maria Giovanna Pavani, Maria Dora Carrion, John A. Hadfield, Pier Giovanni Baraldi, Romeo Romagnoli, Antonietta Di Cristina

Risultato della ricerca: Article

115 Citazioni (Scopus)

Abstract

Two new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene molecular skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. Although many more 3-amino derivatives have been synthesized so far, the most promising compound in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.
Lingua originaleEnglish
pagine (da-a)2273-2277
Numero di pagine5
RivistaJournal of Medicinal Chemistry
Volume50
Stato di pubblicazionePublished - 2007

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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