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

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Remusat, V.
    Carrion, M. D.
    Cara, C. L.
    Cruz-Lopez, O.
    Preti, D.
    Fruttarolo, F.
    Tabrizi, M. A.
    Balzarini, J.
    Hamel, E.

  2. Author Address

    Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA.;Romagnoli, R, Univ Ferrara, Dipartimento Sci Farmaceut, Via Fossato Mortara 17-19, I-44100 Ferrara, Italy.;rmr@unife.it baraldi@unife.it
    1. Year: 2007
    2. Date: Nov
  2. Journal: Medicinal Chemistry
    1. 3
    2. 6
    3. Pages: 507-512
  4. Type of Article: Article
  5. ISSN: 1573-4064
  1. 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.

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External Sources

  1. View record in Web of Science®
  2. WOS: 000250491400001

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