2. Academic Validation
  3. Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization

Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization

  • J Med Chem. 2007 May 3;50(9):2273-7. doi: 10.1021/jm070050f.
Romeo Romagnoli 1,  Pier Giovanni Baraldi,  Maria Dora Carrion,  Carlota Lopez Cara,  Delia Preti,  Francesca Fruttarolo,  Maria Giovanna Pavani,  Mojgan Aghazadeh Tabrizi,  Manlio Tolomeo,  Stefania Grimaudo,  Antonella Di Cristina,  Jan Balzarini,  John A Hadfield,  Andrea Brancale,  Ernest Hamel
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy.
PMID: 17419607 DOI: 10.1021/jm070050f
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.

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