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

@article{Romagnoli2007SynthesisAB,
  title={Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.},
  author={Romeo Romagnoli and Pier Giovanni Baraldi and Maria Dora Carrion and Carlota Lopez Cara and Delia Preti and Francesca Fruttarolo and Maria Giovanna Pavani and Mojgan Aghazadeh Tabrizi and Manlio Tolomeo and Stefania Grimaudo and Antonella Di Cristina and Jan Balzarini and John A. Hadfield and Andrea Brancale and Ernest Hamel},
  journal={Journal of medicinal chemistry},
  year={2007},
  volume={50 9},
  pages={2273-7}
}
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… CONTINUE READING

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