Synthetic Studies of Cortistatin A Analogue from the CD-Ring Fragment of Vitamin D2

Synthetic Studies of Cortistatin A Analogue from the CD-Ring Fragment of Vitamin D2
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DOI:
10.1248/cpb.c13-00375
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发表时间:
2013-10-01
影响因子:
1.7
通讯作者:
Kobayashi, Motomasa
Kobayashi, Motomasa
中科院分区:
医学4区
文献类型:
--
作者:
Kotoku, Naoyuki;Mizushima, Kohei;Kobayashi, Motomasa

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利用维生素 D-2 的 CD 环片段研究了皮质抑素 A (1)(一种来自印度尼西亚海绵的抗血管生成甾体生物碱)的类似化合物的合成。具有CD-顺式融合骨架的新类似物的偶然制备及其生物学评价揭示了CD-转融合结构对于1针对人脐静脉内皮细胞(HUVEC)的有效和选择性抗增殖活性的重要性。
Syntheses of analogue compounds of cortistatin A (1), an anti-angiogenic steroidal alkaloid from Indonesian marine sponge, were investigated by utilizing the CD-ring fragment of vitamin D-2. The incidental preparation of a new analogue having CD-cis-fused skeleton and its biological evaluation revealed the importance of the CD-trans-fused structure for the potent and selective antiproliferative activity of 1 against human umbilical vein endothelial cells (HUVECs).