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
MIGLIO, Gianluca;GENAZZANI A. A.Last
2006-01-01
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.
File in questo prodotto:
| File | Dimensione | Formato | |
|---|---|---|---|
|
2006_Pirali_JMedChem.pdf
Accesso riservato
Tipo di file:
PDF EDITORIALE
Dimensione
109.15 kB
Formato
Adobe PDF
|
109.15 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
