具有有趣细胞毒性活性的新型A环和B环修饰的康普瑞他汀A-4（CA-4）类似物。
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
作者信息
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
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy.
出版信息
J Med Chem. 2008 Oct 9;51(19):6211-5. doi: 10.1021/jm8005004. Epub 2008 Sep 11.
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.
合成了一类新型的秋水仙碱，主要通过用苯并呋喃或苯并[b]噻吩取代对A环或A环和B环进行修饰。新型杂环秋水仙碱对BMEC和H-460细胞系显示出良好的细胞毒性活性。氨基秋水仙碱9f能有效抑制BMEC和对秋水仙碱耐药的HT-29细胞系的细胞生长，对治疗结肠癌具有潜在的意义。杂环秋水仙碱9a、b通过与秋水仙碱位点的结合力比CA-4强五倍，同样能抑制微管蛋白聚合。
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