Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 19, Pages 6211-6215Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm8005004
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Funding
- Ministero dell'Universita e della Ricerca Scientifica e Tecnologica (PRIN 2006), Rome, Italy
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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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