Synthesis and biological evaluation of novel fumagillin and ovalicin analogues.
Synthesis and biological evaluation of novel fumagillin and ovalicin analogues.
复制标题
新型夫马洁林和卵酸类似物的合成和生物学评价。
DOI：
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发表时间：
2005
影响因子：
3.2
通讯作者：
A. Giannis
中科院分区：
文献类型：
--
作者：
Ralph Mazitschek;A. Huwe;A. Giannis
在治愈癌症的众多努力中，一种有希望的方法是中断肿瘤诱导的新血管形成（血管生成）。通过用药物抑制血管生成，肿瘤既不会生长到危及生命的大小，也不会转移。天然产物烟曲霉素1和结构相关的卵蒜素2是两种最有效的抗血管生成化合物。在这里，我们报告的设计和合成的新型烟曲霉素和ovalicin类似物缺乏反应性环氧官能团，这被认为是负责观察到的严重毒副作用。我们还报告了一种新的合成方法和测定这些化合物在内皮细胞中的抗血管生成特性。
A promising approach among the numerous efforts to cure cancer is the interruption of the tumour-induced formation of new blood vessels (angiogenesis). By suppressing angiogenesis with drugs, the tumour can neither grow to a life threatening size, nor metastasize. The natural product fumagillin 1 and the structurally related ovalicin 2 are two of the most potent anti-angiogenic compounds. Here, we report the design and synthesis of novel fumagillin and ovalicin analogues lacking reactive epoxy functionalities, which were thought to be responsible for the severe toxic side-effects observed. We also report a new synthetic approach and the determination of the anti-angiogenic properties of these compounds in endothelial cells.
影响因子：
56.9
作者：
Liu, SP;Widom, J;Clardy, J
通讯作者：
Clardy, J
血管生成调节剂 O-（氯乙酰氨基甲酰基）烟曲霉醇（TNP-470；AGM-1470）在人肝细胞和组织微粒体中的处置和代谢。
影响因子：
11.2
作者：
Placidi,L;Cretton-Scott,E;deSousa,G;Rahmani,R;Placidi,M;Sommadossi,JP
通讯作者：
Sommadossi,JP