Synthesis and Biological Evaluation of 2-amino-3-(3, 4, 5-trimethoxyphenylsulfonyl)-5-aryl thiophenes as a New Class of Antitubulin Agents

Title: Synthesis and Biological Evaluation of 2-amino-3-(3, 4, 5-trimethoxyphenylsulfonyl)-5-aryl thiophenes as a New Class of Antitubulin Agents

Volume: 3 Issue: 6

Author(s): Romeo Romagnoli, Pier Giovanni Baraldi, Vincent Remusat, Maria Dora Carrion, Carlota Lopez Cara, Olga Cruz-Lopez, Delia Preti, Francesca Fruttarolo, Mojgan Aghazadeh Tabrizi, Jan Balzarini and Ernest Hamel

Affiliation:

Keywords: Microtubule, combretastatin A-4, bioisoster, 2-aminothiophene

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.

Cite this article as:

Romagnoli Romeo, Baraldi Giovanni Pier, Remusat Vincent, Carrion Dora Maria, Cara Lopez Carlota, Cruz-Lopez Olga, Preti Delia, Fruttarolo Francesca, Tabrizi Aghazadeh Mojgan, Balzarini Jan and Hamel Ernest, Synthesis and Biological Evaluation of 2-amino-3-(3, 4, 5-trimethoxyphenylsulfonyl)-5-aryl thiophenes as a New Class of Antitubulin Agents, Medicinal Chemistry 2007; 3 (6) . https://dx.doi.org/10.2174/157340607782360380