Two new series of inhibitors of tubulin polymn. based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene mol. skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymn., and cell cycle effects. Although many more 3-amino derivs. have been synthesized so far, the most promising compd. in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concns. and interacts strongly with tubulin by binding to the colchicine site.

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

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;FRUTTAROLO, Francesca;PAVANI, Maria Giovanna;AGHAZADEH TABRIZI, Mojgan;
2007

Abstract

Two new series of inhibitors of tubulin polymn. based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene mol. skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymn., and cell cycle effects. Although many more 3-amino derivs. have been synthesized so far, the most promising compd. in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concns. and interacts strongly with tubulin by binding to the colchicine site.
2007
Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Md; Cara, Cl; Preti, Delia; Fruttarolo, Francesca; Pavani, Maria Giovanna; AGHAZADEH TABRIZI, Mojgan; Tolomeo, M; Grimaudo, S; DI CRISTINA, A; Balzarini, J; Hadfield, Ja; Brancale, A; Hamel, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/471428
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