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N-烷酰基-S-苄基-L-半胱氨酰谷氨酸酯作为乙二醛酶I抑制剂和抗癌剂的合成与评价

Synthesis and evaluation of N-alkanoyl-S-benzyl-L-cysteinylglutamic acid esters as glyoxalase I inhibitors and anticancer agents.

作者信息

Foye W O, Jan C M

出版信息

J Pharm Sci. 1984 Apr;73(4):559-61. doi: 10.1002/jps.2600730431.

DOI:10.1002/jps.2600730431
PMID:6726645
Abstract

Esters of several glutathione analogues have been synthesized in which the glycine moiety was replaced by straight-chain fatty acids and the mercapto group was benzylated . Two of the derivatives (sufficiently water-soluble for the assay) were found to inhibit glyoxalase I to a greater extent than did S-methylglutathione. The two glyoxalase I inhibitors did not inhibit P388 lymphocytic leukemia in mice, however.

摘要

已经合成了几种谷胱甘肽类似物的酯，其中甘氨酸部分被直链脂肪酸取代，巯基被苄基化。发现其中两种衍生物（水溶性足以用于该测定）比S-甲基谷胱甘肽更能抑制乙二醛酶I。然而，这两种乙二醛酶I抑制剂并未抑制小鼠的P388淋巴细胞白血病。

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