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.File in questo prodotto:
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