Title: Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Jung, M Katherine
Iaconinoto, Maria Antonietta
Carrion, Maria Dora
Remusat, Vincent
Preti, Delia
Tabrizi, Mojgan Aghazadeh
Francesca, Fruttarolo
De Clercq, Erik
Balzarini, Jan
Hamel, Ernest #
Issue Date: Sep-2005
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:15 issue:18 pages:4048-4052
Abstract: A new series of compounds, in which the 2-amino-4-methoxyphenyl ring of phenstatin analogue 5 was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivatives (8 and 9, respectively) indicates that the 3',4',5'-trimethoxybenzoyl moiety is critical for the activity. Two compounds, 7 and 11, displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Derivative 11 was more active than CA-4 as an inhibitor of tubulin polymerization. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymerization.
ISSN: 0960-894X
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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