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

作者：Simoni Daniele^*; Romagnoli Romeo; Baruchello Riccardo; Rondanin Riccardo; Grisolia Giuseppina; Eleopra Marco; Rizzi Michele; Tolomeo Manlio; Giannini Giuseppe; Alloatti Domenico; Castorina Massimo; Marcellini Marcella; Pisano Claudio

来源：Journal of Medicinal Chemistry, 2008, 51(19): 6211-6215.

DOI：10.1021/jm8005004

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.

• 出版日期2008-10-9