Bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compds. into safer and more clin. effective agents. Bioisosteres are substituents or groups that have chem. or phys. similarities and that produce broadly similar biol. effects. The sulfone moiety is recognized as a nonclassical bioisostere for replacement of the carbonyl group. When sulfonyl derivs. 5a-e were compared with carbonyl compds. 4a-e, the sulfone substitution dramatically decreased the antiproliferative activity of the series.

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

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;FRUTTAROLO, Francesca;AGHAZADEH TABRIZI, Mojgan;
2007

Abstract

Bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compds. into safer and more clin. effective agents. Bioisosteres are substituents or groups that have chem. or phys. similarities and that produce broadly similar biol. effects. The sulfone moiety is recognized as a nonclassical bioisostere for replacement of the carbonyl group. When sulfonyl derivs. 5a-e were compared with carbonyl compds. 4a-e, the sulfone substitution dramatically decreased the antiproliferative activity of the series.
2007
Romagnoli, Romeo; Baraldi, Pier Giovanni; Remusat, V; Carrion, M. D.; Lopez Cara, C.; Cruz Lopez, O; Preti, Delia; Fruttarolo, Francesca; AGHAZADEH TA...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/517677
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