2-(3',4',5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivs., e.g., I, were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymn., and cell cycle effects. SARs were elucidated with various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para-position of the 5-Ph group showed antiproliferative activity in the order of F:CH3 > OCH3:Br:NO2 > CF3:I > OEt. Several of these compds. led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis.

Synthesis and biological evaluation of 2-(3 ',4 ',5 '-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;FRUTTAROLO, Francesca;PAVANI, Maria Giovanna;AGHAZADEH TABRIZI, Mojgan;
2006

Abstract

2-(3',4',5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivs., e.g., I, were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymn., and cell cycle effects. SARs were elucidated with various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para-position of the 5-Ph group showed antiproliferative activity in the order of F:CH3 > OCH3:Br:NO2 > CF3:I > OEt. Several of these compds. led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis.
2006
Romagnoli, Romeo; Baraldi, Pier Giovanni; Remusat, V; Carrion, Md; Cara, Cl; Preti, Delia; Fruttarolo, Francesca; Pavani, Maria Giovanna; AGHAZADEH TABRIZI, Mojgan; Tolomeo, M; Grimaudo, S; Balzarini, J; Jordan, Ma; Hamel, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/495446
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