Title: Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Remusat, Vincent
Carrion, Maria Dora
Cara, Carlota Lopez
Preti, Delia
Fruttarolo, Francesca
Pavani, Maria Giovanna
Tabrizi, Mojgan Aghazadeh
Tolomeo, Manlio
Grimaudo, Stefania
Balzarini, Jan
Jordan, Mary Ann
Hamel, Ernest #
Issue Date: Oct-2006
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:49 issue:21 pages:6425-6428
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 F=CH(3) > OCH(3)=Br=NO(2) > CF(3)=I > 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.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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