Structure-activity relationships study of bastadin 6, an anti-angiogenic brominated-tyrosine derived metabolite from marine sponge
Structure-activity relationships study of bastadin 6, an anti-angiogenic brominated-tyrosine derived metabolite from marine sponge
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DOI：
10.1002/ardp.200700231
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发表时间：
2008-09-01
影响因子：
5.1
通讯作者：
Kobayashi, Motomasa
中科院分区：
文献类型：
--
作者：
Kotoku, Naoyuki;Hiramatsu, Atsushi;Kobayashi, Motomasa
对从印尼海绵中提取的具有抗血管生成活性的溴化酪氨酸代谢物巴斯塔丁6(1)进行了构效关系(SAR)研究。酮修饰的类似物和溴修饰的类似物的合成和生物学评价表明，在显示对人脐静脉内皮细胞(HUVECs)的有效和选择性的抗增殖活性方面，BASTADIN 6(1)中的肟部分和溴原子都具有重要的作用。
A structure-activity relationship (SAR) study of bastadin 6 (1), a brominated tyrosine-derived metabolite from Indonesian marine sponge having a potent anti-angiogenic activity, was executed. The syntheses and their biological evaluation of the oxime-modified analogues and bromine-modified analogues revealed that both the oxime moieties and bromine atoms in bastadin 6 (1) play an important role to show the potent and selective anti-proliferative activity against human umbilical vein endothelial cells (HUVECs).