| Identification | Back Directory | [Name]
L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride | [CAS]
221174-33-0 | [Synonyms]
L-gamma-Glutamyl-S-[[(4-bromophenyl)hydroxyamino]carbonyl]-L-cysteinylglycine diethyl ester monohydrochloride
Glycine, L-γ-glutaMyl-S-[[(4-broMophenyl)hydroxyaMino]carbonyl]-L-cysteinyl-, diethyl ester, Monohydrochloride (9CI)
ethyl (2S)-2-amino-5-[[(2R)-3-[(4-bromophenyl)-hydroxycarbamoyl]sulfanyl-1-[(2-ethoxy-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate | [Molecular Formula]
C21H29BrN4O8S.HCl | [MDL Number]
MFCD20270724 | [MOL File]
221174-33-0.mol | [Molecular Weight]
613.907 |
| Hazard Information | Back Directory | [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. |
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SPIRO PHARMA
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Musechem
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BOC Sciences
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