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.
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Data di pubblicazione: | 2008 | |
Titolo: | Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity. | |
Autori: | Daniele Simoni; Romeo Romagnoli; Riccardo Baruchello; Riccardo Rondanin; Giuseppina Grisolia; Marco Eleopra; Michele Rizzi; Manlio Tolomeo; Giuseppe Giannini; Domenico Alloatti; Massimo Castorina; Marcella Marcellini; Claudio Pisano | |
Rivista: | JOURNAL OF MEDICINAL CHEMISTRY | |
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. | |
Handle: | http://hdl.handle.net/11392/529727 | |
Appare nelle tipologie: | 03.1 Articolo su rivista |