Novel A-Ring and B-Ring Modified Combretastatin A-4 (CA-4) Analogues Endowed with Interesting Cytotoxic Activity
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- 作者：Daniele Simoni ; Romeo Romagnoli ; Riccardo Baruchello ; Riccardo Rondanin ; Giuseppina Grisolia ; Marco Eleopra ; Michele Rizzi ; Manlio Tolomeo ; Giuseppe Giannini ; Domenico Alloatti ; Massimo Castorina ; Mar
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：October 9, 2008
- 年：2008
- 卷：51
- 期：19
- 页码：6211-6215
- 全文大小：129K
- 年卷期：v.51,no.19(October 9, 2008)
- ISSN：1520-4804
文摘
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.