Semisynthesis of an analogue of antitumor bicyclic hexapeptide RA-VII by fixing the Ala-2/Tyr-3 bond to cis by incorporating a triazole cis-amide bond surrogate
Semisynthesis of an analogue of antitumor bicyclic hexapeptide RA-VII by fixing the Ala-2/Tyr-3 bond to cis by incorporating a triazole cis-amide bond surrogate
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DOI：
10.1021/ol040005r
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发表时间：
2004-04-01
期刊：
影响因子：
5.2
通讯作者：
Takeya, K
中科院分区：
文献类型：
--
作者：
Hitotsuyanagi, Y;Motegi, S;Takeya, K
我们制备了抗肿瘤双环六肽RA-VII的类似物，其残基2和3之间的酰胺构型通过掺入三唑顺式酰胺键替代物固定为顺式。这种类似物显示，通过NMR研究，采取几乎相同的构象的RA-VII的次要构象。它没有表现出细胞毒活性。
We prepared an analogue of an antitumor bicyclic hexapeptide RA-VII whose amide configuration between residues 2 and 3 was fixed to cis by incorporating a triazole cis-amide bond surrogate. This analogue was shown, by NMR studies, to take almost the same conformation as that of the minor conformer of RA-VII. It showed no cytotoxic activity.