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

[ Vol. 3 , Issue. 6 ]


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   Pages 507 - 512 ( 6 )


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.


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


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

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