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Synthesis and biological evaluation of 2-amino-3-(3', 4', 5'-trimethoxy-phenylsulfonyl)-5-aryl thiophenes as a new class of antitubulin agents.

作者信息

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

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, I-44100 Ferrara, Italy.

出版信息

Med Chem. 2007 Nov;3(6):507-12. doi: 10.2174/157340607782360380.

DOI:10.2174/157340607782360380
PMID:18045199
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.

摘要

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