We have synthesized rigid analogues of combretastatin bearing a furan ring in place of the olefinic bridge. These compounds are cytotoxic at nanomolar concentrations in neuroblastoma cells, display a similar structure- activity relationship compared to combretastatin A4, and inhibit tubulin polymerization. We also show that the furan ring can be further functionalized. Thus, it is possible that combretafurans could act as scaffolds for the development of dual-action antitumoral agents.
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents / T. Pirali, S. Busacca, L. Beltrami, D. Imovilli, F. Pagliai, G. Miglio, A. Massarotti, L. Verotta, G.C. Tron, G. Sorba, A.A. Genazzani. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 49:17(2006 Jul 29), pp. 5372-5376.
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents
L. Verotta;
2006
Abstract
We have synthesized rigid analogues of combretastatin bearing a furan ring in place of the olefinic bridge. These compounds are cytotoxic at nanomolar concentrations in neuroblastoma cells, display a similar structure- activity relationship compared to combretastatin A4, and inhibit tubulin polymerization. We also show that the furan ring can be further functionalized. Thus, it is possible that combretafurans could act as scaffolds for the development of dual-action antitumoral agents.
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