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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, P.; Remusat, V.; Carrion, M.; Cara, C.; Preti, D.; Fruttarolo, F.; Pavani, M.; Tabrizi, M.; Tolomeo, M.; Grimaudo, S.; Balzarini, J.; Jordan, M.; Hamel, E.
  • Anno di pubblicazione: 2006
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • OA Link:


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.