Title: Synthesis and biological evaluation of 2-amino-3-(3', 4', 5'-trimethoxy-phenylsulfonyl)-5-aryl thiophenes as a new class of antitubulin agents
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Remusat, Vincent
Carrion, Maria Dora
Cara, Carlota Lopez
Cruz-Lopez, Olga
Preti, Delia
Fruttarolo, Francesca
Tabrizi, Mojgan Aghazadeh
Balzarini, Jan
Hamel, Ernest #
Issue Date: 13-Nov-2007
Publisher: Bentham science publ ltd.
Series Title: Medicinal Chemistry vol:3 issue:6 pages:507-512
Abstract: Bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compounds into safer and more clinically effective agents. Bioisosteres are substituents or groups that have chemical or physical similarities and that produce broadly similar biological effects. The sulfone moiety is recognized as a nonclassical bioisostere for replacement of the carbonyl group. When sulfonyl derivatives 5a-e were compared with carbonyl compounds 4a-e, the sulfone substitution dramatically decreased the antiproliferative activity of the series.
ISSN: 1573-4064
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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