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

Stefania Grimaudo, Carlota Lopez Cara, Ernest Hamel, Mojgan Aghazadeh Tabrizi, Jan Balzarini, Mary Ann Jordan, Francesca Fruttarolo, Vincent Remusat, Delia Preti, Maria Giovanna Pavani, Maria Dora Carrion, Pier Giovanni Baraldi, Romeo Romagnoli

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Abstract

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.
Original languageEnglish
Pages (from-to)6425-6428
Number of pages4
JournalJournal of Medicinal Chemistry
Volume49
Publication statusPublished - 2006

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All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Grimaudo, S., Lopez Cara, C., Hamel, E., Aghazadeh Tabrizi, M., Balzarini, J., Jordan, M. A., Fruttarolo, F., Remusat, V., Preti, D., Pavani, M. G., Carrion, M. D., Baraldi, P. G., & Romagnoli, R. (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, 49, 6425-6428.