| Autor: |
Thornalley PJ; Department of Biological and Chemical Sciences, University of Essex, Colchester, U.K., Ladan MJ, Ridgway SJ, Kang Y |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1996 Aug 16; Vol. 39 (17), pp. 3409-11. |
| DOI: |
10.1021/jm960129c |
| Abstrakt: |
S-(p-Bromobenzyl)glutathione is a competitive inhibitor of human glyoxalase I which is part of the cytosolic glyoxalase system. It may be delivered into the cystosol of cells by diesterification wherein it is deesterified by cytosolic nonspecific esterases. S-(p-Bromobenzyl)glutathione diesters had antitumor activity in vitro and in vivo. The inhibition of human leukemia 60 cell growth in vitro by a series of alkyl and cycloalkyl diesters of S-(p-bromobenzyl)glutathione was investigated. For n-alkyl diesters, the n-propyl diester was the most potent derivative with a median growth inhibitory concentration GC50 value of 7.77 +/- 0.01 microM (N = 18). The most potent derivative was S-(p-bromobenzyl)glutathione cyclopentyl diester which had a GC50 value of 4.23 +/- 0.01 microM (N = 21) and also had antitumor activity in vivo. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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