Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents

J Med Chem. 2006 Aug 24;49(17):5372-6. doi: 10.1021/jm060621o.

Tracey Pirali ¹, Sara Busacca, Lorena Beltrami, Daniela Imovilli, Francesca Pagliai, Gianluca Miglio, Alberto Massarotti, Luisella Verotta, Gian Cesare Tron, Giovanni Sorba, Armando A Genazzani

Affiliations

Affiliation

1 Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center, Università degli Studi del Piemonte Orientale A. Avogadro, Via Bovio 6, 28100 Novara, Italy.

PMID: 16913727 DOI: 10.1021/jm060621o

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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