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flucorcombretastatin and derivatives thereof

机译:氟考贝他汀及其衍生物

摘要

"FLUORCOMBRETASTATIN AND DERIVATIVES THEREOF". The present invention relates to novel combretastatin derivatives of formula (I) obtained by total synthesis. The strategy developed for each of the compounds is i) to replace hydrogen with a halogen (ie fluorine atom) in the olefin bond; ii) replacing an aromatic ring in a natural product with an amino aromatic ring. Said compounds recognize and bind to the tubulin site; They are useful for treating disease states that result from cell proliferation or are exacerbated by cell proliferation - such as anticancer and / or antiangiogenic activity in a mammal - for pharmaceutical compositions comprising such compounds.
机译:“氟康他汀及其衍生物”。通过全合成获得的式(I)的新型康维他汀衍生物。为每种化合物开发的策略是:i)用烯烃键中的卤素(即氟原子)代替氢; ii)用氨基芳族环取代天然产物中的芳族环。所述化合物识别并结合微管蛋白位点;它们可用于治疗由细胞增殖引起的或因细胞增殖而加剧的疾病状态,例如哺乳动物中的抗癌和/或抗血管生成活性,用于包含此类化合物的药物组合物。

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