Corpus ID: 25197702

Radiosensitizing effect of 2,4-dinitroimidazole-1-ethanol and its cytotoxicity in HeLa S3 cells.

  title={Radiosensitizing effect of 2,4-dinitroimidazole-1-ethanol and its cytotoxicity in HeLa S3 cells.},
  author={C. Shibata and H. Hori and S. Inayama and T. Mori},
  volume={157 7},
Using cultured HeLa S3 cells, the radiosensitizing and cytotoxic effects of newly synthesized derivatives of dinitroimidazole were investigated and compared with those of misonidazole. 2,4-Dinitroimidazole-1-ethanol radiosensitized hypoxic cells selectively. At 5 mM misonidazole, the enhancement ratio was 1.95; with 0.5 mM 2,4-dinitroimidazole-1-ethanol, almost the same enhancement could be obtained. This indicates that the radiosensitizing effect of the latter agent was about 10 times greater… Expand
10 Citations
2-Arylidene-4-cyclopentene-1,3-diones designed as non-nitro radiosensitizers and hypoxic cytotoxins.
The radiosensitizing effects and hypoxic cytotoxicity of 2-(4'-hydroxybenzylidene)-cyclopentene-1,3-dione and its 3'-methoxy and 3',5'-dimethoxy derivatives were investigated in vitro and showed to have weak but apparentHypoxic cells were more sensitive than aerobic cells at very low drug concentrations (below 10 microM), whereas KIH-200 was less effective. Expand
Cytotoxic properties of hydroxylamino- and amino-misonidazole, possible metabolic products of misonidazole, in hypoxic HeLa S3 cells.
After a 3-hr exposure to 1mM hydroxylaminomisonidazole under aerobic and hypoxic conditions, the surviving cell fractions were 0.18 and 0.0056, which represents a cytotoxicity five and 125 times greater, respectively, than that of misonidrazole. Expand
Radiosensitization by a new nucleoside analogue: 1-[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl-2-nitroimidazole (RP-170).
In vivo-in vitro excision analysis showed that RP-170 was also as effective as MISO and etanidazole to radiosensitize solid tumor cells in vivo and might be preferable under certain circumstances because it can be given orally. Expand
Radiosensitization by a new potent nucleoside analog: 1-(1',3',4'-trihydroxy-2'-butoxy)methyl-2-nitroimidazole(RP-343).
RP-343 was found to have better sensitization of solid tumors over both etanidazole and RP-170, and the effectively lower therapeutic risk index for RP-343 presents the possibility of clinical advantage over etanodazole. Expand
Radiosensitization of hypoxic HeLa S3 cells in vitro by a new type of radiosensitizer: spermine and spermidine amides with nitro groups.
Among them, N1, N10-bis(4-nitrobenzoyl)-spermidine (FNT-1) was most effective and suggested to play an important role in sensitization. Expand
Effect of arylidene-cyclopentenedione radiosensitizers on ATP synthesis in mitochondria: action as potent inhibitors of phosphate transport.
The effects of the arylidene-cyclopentenedione radiosensitizers, KIH-200, 201 and 202 on ATP synthesis in mitochondria were examined and these three compounds were found to have very potent inhibitory effects on Pi-transport into mitochondria. Expand
Development of new hypoxic cell sensitizers: Amides of nitrobenzoic acid with spermidine and spermine
New type hypoxic cell sensitizers, N1, N10-bis(4-nitrobenzoyl)spermidine and N1-N14-bis-spermine, were developed and were shown to be more effective radiosensitizers to hypoxic cells than misonidazole. Expand
An in vitro and in vivo screening system for new hypoxic cell radiosensitizers using EMT6 cells.
An experimental tumor system consisting of single cells, spheroids, and solid tumors was developed using the EMT6/KU cell-line for evaluation of new hypoxic cell sensitizers and it was suggested that an efficient sensitizer in vivo shows little or no difference between its ER for single cells and that for sp Heroids. Expand
Effect of hypoxic cell radiosensitizers on glutathione level and related enzyme activities in isolated rat hepatocytes.
Addition of partially purified glutathione S-transferase (GST) did not enhance DNIE-mediated GSH loss in a cell-free system, while misonidazole and KIH-3 did not. Expand
Design, synthesis, and biological activity of anti-angiogenic hypoxic cell radiosensitizer haloacetylcarbamoyl-2-nitroimidazoles.
The in vivo chick CAM angiogenesis assay showed that the strong bromoacetylcarbamoyl-2-nitroimidazole radiosensitizers, such as TX-1845 andTX-1846, were the strongest angiogenic inhibitors among them. Expand