Glyoxalase I enzyme studies. 3. Synthesis and evaluation of .alpha.-hydroxythiol esters as antitumor agents and glyoxalase I inhibitors

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Abstract
Synthesis of a series of .alpha.-hydroxythiol esters made available, for the 1st time, product-like molecules that were evaluated as inhibitors of the enzyme glyoxalase I [S-lactoylglutathione methylglyoxal lyase, EC 4.4.1.5] and as potential antitumor agents. All the .alpha.-hydroxythiol esters tested were competitive inhibitors of the enzyme, albeit weak; the relative [I]50 [median inhibitory] values suggested information about the active site. Antileukemic activity in L1210 lymphoid leukemia [mouse] indicated no significant activity by these .alpha.-hydroxythiol esters.
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