TY - JOUR
T1 - Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AU - Grimaudo, Stefania
AU - Lopez Cara, Carlota
AU - Hamel, Ernest
AU - Aghazadeh Tabrizi, Mojgan
AU - Balzarini, Jan
AU - Jordan, Mary Ann
AU - Fruttarolo, Francesca
AU - Remusat, Vincent
AU - Preti, Delia
AU - Pavani, Maria Giovanna
AU - Carrion, Maria Dora
AU - Baraldi, Pier Giovanni
AU - Romagnoli, Romeo
PY - 2006
Y1 - 2006
N2 - 2-(3‘,4‘,5‘-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, 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-phenyl group showed antiproliferative activity in the order of FCH3 > OCH3BrNO2 > CF3I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis.
AB - 2-(3‘,4‘,5‘-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, 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-phenyl group showed antiproliferative activity in the order of FCH3 > OCH3BrNO2 > CF3I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis.
UR - http://hdl.handle.net/10447/6273
M3 - Article
SN - 0022-2623
VL - 49
SP - 6425
EP - 6428
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
ER -