Thornalley P J, Ladan M J, Ridgway S J, Kang Y
Department of Biological and Chemical Sciences, University of Essex, Colchester, U.K.
J Med Chem. 1996 Aug 16;39(17):3409-11. doi: 10.1021/jm960129c.
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.
S-（对溴苄基）谷胱甘肽是人体乙二醛酶I的竞争性抑制剂，乙二醛酶I是胞质乙二醛酶系统的一部分。它可通过二酯化作用被递送至细胞胞质溶胶中，在那里它会被胞质非特异性酯酶去酯化。S-（对溴苄基）谷胱甘肽二酯在体外和体内均具有抗肿瘤活性。研究了一系列S-（对溴苄基）谷胱甘肽的烷基和环烷基二酯对人白血病60细胞体外生长的抑制作用。对于正烷基二酯，正丙基二酯是最有效的衍生物，其半数生长抑制浓度GC50值为7.77±0.01微摩尔（N = 18）。最有效的衍生物是S-（对溴苄基）谷胱甘肽环戊基二酯，其GC值为4.23±0.01微摩尔（N = 21），并且在体内也具有抗肿瘤活性。 50
