Synthesis and Cytotoxic Evaluation of Combretafurans, Potential Scaffolds for Dual-Action Antitumoral Agents
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- 作者：Tracey Pirali ; Sara Busacca ; Lorena Beltrami ; Daniela Imovilli ; Francesca Pagliai ; Gianluca Miglio ; Alberto Massarotti ; Luisella Verotta ; Gian Cesare Tron ; Giovanni Sorba ; Armando A. Genazzani
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：August 24, 2006
- 年：2006
- 卷：49
- 期：17
- 页码：5372 - 5376
- 全文大小：109K
- 年卷期：v.49,no.17(August 24, 2006)
- ISSN：1520-4804
文摘
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 similarstructure-activity relationship compared to combretastatin A4, and inhibit tubulin polymerization. We alsoshow that the furan ring can be further functionalized. Thus, it is possible that combretafurans could act asscaffolds for the development of dual-action antitumoral agents.