专利号:US-7572778-B2 优先权日:2003-07-18 标题 :Fluorocombretastatin and derivatives thereof 发明人:GIANNINI GIUSEPPE; ALLOATTI DOMENICO; MARCELLINI MARCELLA; MARZI MAURO; RICCIONI TERESA; TINTI MARIA ORNELLA 权利人:SIGMA TAU IND FARMACEUTI 摘要:The present invention is related to new derivatives of Combretastatin, of Formula n nobtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation—as anticancer and/or antiangiogenic activity, in a mammal—to pharmaceutical compositions comprising these compounds.