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Design, Synthesis and Evaluation of Antitumor Activity against Human Cancer Cell Lines,Sansalvamide Analogues

机译:抗肿瘤性抗肿瘤性抗肿瘤活性的设计,合成与评价,桑拉酰胺类似物

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@@ Sansalvamide A[1] (1) is a cyclic depsipeptide produced by a marine fungus of the genus Fusarium (Fusarium ssp.), this compound was found to possess significant cancer cell cytotoxicity. We have synthesized the corresponding cyclic peptide[2] of sansalvamide A (2), which is the amide derivative of sansalvamide A. Previous work of our group demonstrated that the antitumor activity of peptide sansalvamide A (2) is ten times more potent than Sansalvamide A (1), and the N-methylation of amino acid is also effect on antitumor activity, such as compound (3)[3] (Figure 1).
机译:@@ sansalvamide a [1](1)是由镰刀菌属(镰刀菌镰刀菌)的海洋真菌产生的循环脂肪肽。发现该化合物具有显着的癌细胞细胞毒性。我们合成了桑拉凡柳酰胺A(2)的相应环状肽[2],这是桑拉柳酰胺A的酰胺衍生物。我们的小组的先前工作表明,肽Sansalvamide A(2)的抗肿瘤活性比桑拉酰胺更有效的抗肿瘤活性(1),氨基酸的N-甲基化也对抗肿瘤活性效果,例如化合物(3)[3](图1)。

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