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| L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride Basic information |
| L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride Chemical Properties |
storage temp. | 4°C, protect from light, stored under nitrogen | solubility | Soluble in DMSO | form | Powder |
| L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride Usage And Synthesis |
Biological Activity | s-(n-aryl-n-hydroxycarbamoyl)glutathione derivatives have been proposed as possible anticancer agents, because of their ability to strongly inhibit the methylglyoxal-detoxifying enzyme glyoxalase i. glyoxalase i inhibitor is a potent inhibitor of glyoxalase i. | in vitro | as a tumor-selective anticancer agent, glyoxalase i inhibitor [3(et)2] was evaluated against b16 melanotic melanoma, l1210 murine leukemia, and nonproliferating murine splenic lymphocytes in culture. the diethyl ester prodrugs of glyoxalase i inhibitor [3(et)2] also displayed significant tumour-selective toxicity towards l1210 cells compared with normal murine splenic lymphocytes in vitro [1]. | in vivo | small-scale efficacy studies indicated that 3b(et)2 could effectively inhibit tumour growth in plasma esterase-deficient mice bearing murine b16 melanoma and in esterasedeficient athymic nude mice bearing androgen-independent human prostate pc-3 tumours or human colon ht-29 tumours [2]. | target | glyoxalase I | references | [1] kavarana mj, kovaleva eg, creighton dj, wollman mb, eiseman jl. mechanism-based competitive inhibitors of glyoxalase i: intracellular delivery, in vitro antitumor activities, and stabilities in human serum and mouse serum. j med chem. 1999;42(2):221-8. [2] creighton dj, zheng zb, holewinski r, hamilton ds, eiseman jl. glyoxalase i inhibitors in cancer chemotherapy. biochem soc trans. 2003;31(pt 6):1378-82. |
| L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride Preparation Products And Raw materials |
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