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基于2,3-断-1-氰基-19β,28-环氧-18α-齐墩果-3-烯酸的三萜酰胺的合成

[The synthesis of triterpenic amides based on 2,3-seco-1-cyano-19beta,28-epoxy-18alpha-olean-3-oic acid].

作者信息

Tolmacheva I A, Igosheva E V, Grishko V V, Zhukova O S, Gerasimova G K

出版信息

Bioorg Khim. 2010 May-Jun;36(3):410-5. doi: 10.1134/s1068162010030143.

Abstract

Novel 2,3-seco-triterpenic amides were prepared by the interaction of the chloride of 2,3-seco-l-cyano-19beta,28-epoxy-18alpha-oleane-3-oic acid with primary amines and synthetic and biogenic amino acids. A cytotoxic triterpenic conjugate with a residue of the ethyl ester of beta-alanine was found among the synthesized nitrogen-containing derivatives. Treatment with this conjugate in a concentration of 100 muM resulted in the 45.5% survival of melanoma cells in the medium.

摘要

通过2,3-断-1-氰基-19β,28-环氧-18α-齐墩果-3-烯酸的氯化物与伯胺以及合成和生物源氨基酸的相互作用制备了新型2,3-断三萜酰胺。在合成的含氮衍生物中发现了一种带有β-丙氨酸乙酯残基的细胞毒性三萜共轭物。用浓度为100μM的这种共轭物处理导致培养基中黑色素瘤细胞的存活率为45.5%。

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