α-羟基硫醇酯作为抗肿瘤剂和乙二醛酶I抑制剂的合成与评价

Synthesis and evaluation of alpha-hydroxythiol esters as antitumor agents and glyoxalase I inhibitors.

作者信息

Hall S S, Doweyko L M, Doweyko A M, Zilenovski J S

出版信息

J Med Chem. 1977 Oct;20(10):1239-42. doi: 10.1021/jm00220a002.

Abstract

Synthesis of a series of alpha-hydroxythiol esters made available, for the first time, product-like molecules that were evaluated as inhibitors of the enzyme glyoxalase I and as potential antitumor agents. All the alpha-hydroxythiol esters tested were competitive inhibitors of the enzyme, albeit weak; however, the relative [I]50 values suggested information about the active site. Antileukemic activity in L1210 lymphoid leukemia indicated no significant activity by these alpha-hydroxythiol esters.

摘要

一系列α-羟基硫醇酯的合成首次提供了类似产物的分子，这些分子被评估为乙二醛酶I的抑制剂和潜在的抗肿瘤剂。所有测试的α-羟基硫醇酯都是该酶的竞争性抑制剂，尽管作用较弱；然而，相对的[I]50值提供了有关活性位点的信息。在L1210淋巴细胞白血病中的抗白血病活性表明这些α-羟基硫醇酯没有显著活性。