Bastadins, cyclic tetramers of brominated-tyrosine derivatives, selectively inhibit the proliferation of endothelial cells

Bastadins, cyclic tetramers of brominated-tyrosine derivatives, selectively inhibit the proliferation of endothelial cells
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DOI:
10.1007/s11418-006-0045-3
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发表时间:
2006-01-01
影响因子:
3.3
通讯作者:
Kobayashi, Motomasa
Kobayashi, Motomasa
中科院分区:
医学3区
文献类型:
--
作者:
Aoki, Shunji;Cho, Seok-hwan;Kobayashi, Motomasa

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从海绵底孢虫中分离得到8个溴化酪氨酸衍生物四聚体,并测定了它们对内皮细胞的抗增殖活性。对这些化合物的构效关系研究表明,大环结构是至关重要的,而bastadins型骨架对于这些bastadins对内皮细胞的选择性活性是重要的。并通过分子力学计算对其构象进行了分析。
Eight bastadins, tetramers of brominatedtyrosine derivatives, were isolated from the marine sponge Ianthella basta, and their anti-proliferative activities against endothelial cells were examined. A structure-activity relationship study of these compounds revealed that a macrocyclic structure was crucial, and a bastarane-type skeleton was important for the selective activity of these bastadins against endothelial cells. A conformational analysis of the bastadins was also carried out by molecular mechanics calculation.