831222-80-1Relevant academic research and scientific papers
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, Michèle,Tolomeo, Manlio,Giannini, Giuseppe,Alloatti, Domenico,Castorina, Massimo,Marcellini, Marcella,Pisano, Claudio
supporting information; experimental part, p. 6211 - 6215 (2009/10/23)
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.
COMBRETASTATIN DERIVATIVES WITH CYTOTOXIC ACTION
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Page 38; 39-40, (2010/02/10)
The invention described herein relates to new combretastatin derivatives obtained by total synthesis and having the following general formula (I) in which the groups are as defined in the description here below. Said compounds, though chemically related to the structure of cis/trans-combretastatin, do not always bind tubulin, but nevertheless exhibit cytotoxic activity of interest in the oncological field as anticancer and/or antiangiogenic agents.
