A novel class of combretastatins, modified at A-ring or both A- and B-rings, mainly by replacement with benzofuran or benzo[b]thiophene, were synthesized. The new heterocombretastatins showed good cytotoxic activity on BMEC and H-460 cell lines. The aminocombretastatin 9f potently inhibits cell growth of BMEC and combretastatin-resistant HT-29 cell lines, with potential interest to treat colon carcinoma. Heterocombretastatins 9a,b inhibit tubulin polymerization similarly to CA-4 by having a binding to colchicine site five times stronger.

Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.

SIMONI, Daniele;ROMAGNOLI, Romeo;BARUCHELLO, Riccardo;RONDANIN, Riccardo;GRISOLIA, Giuseppina;ELEOPRA, Marco;RIZZI, Michele;
2008

Abstract

A novel class of combretastatins, modified at A-ring or both A- and B-rings, mainly by replacement with benzofuran or benzo[b]thiophene, were synthesized. The new heterocombretastatins showed good cytotoxic activity on BMEC and H-460 cell lines. The aminocombretastatin 9f potently inhibits cell growth of BMEC and combretastatin-resistant HT-29 cell lines, with potential interest to treat colon carcinoma. Heterocombretastatins 9a,b inhibit tubulin polymerization similarly to CA-4 by having a binding to colchicine site five times stronger.
Simoni, Daniele; Romagnoli, Romeo; Baruchello, Riccardo; Rondanin, Riccardo; Grisolia, Giuseppina; Eleopra, Marco; Rizzi, Michele; Manlio, Tolomeo; Giuseppe, Giannini; Domenico, Alloatti; Massimo, Castorina; Marcella, Marcellini; Claudio, Pisano
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/529727
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