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.
|Data di pubblicazione:||2006|
|Titolo:||Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.|
|Autori:||ROMAGNOLI R; BARALDI PG; REMUSAT V; CARRION MD; CARA CL; PRETI D; FRUTTAROLO F; PAVANI MG; TABRIZI MA; TOLOMEO M; GRIMAUDO S; BALZARINI J; JORDAN MA; HAMEL E|
|Tipologia:||Articolo su rivista|
|Citazione:||ROMAGNOLI R, BARALDI PG, REMUSAT V, CARRION MD, CARA CL, PRETI D, et al. (2006). Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, Oct 19;49(21), 6425-6428.|
|Digital Object Identifier (DOI):||10.1021/jm060804a|
|Appare nelle tipologie:||01 - Articolo su rivista|