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.File in questo prodotto:
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