2004
DOI: 10.1016/j.bmcl.2004.02.060
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Propargylic sulfones possessing a 2-nitroimidazole function: novel hypoxic-cell radiosensitizers with intracellular non-protein thiol depletion ability

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Cited by 6 publications
(3 citation statements)
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“…[1][2][3][4][5] Hypoxic cells have been recognized to show resistance to ionizing radiation, the biological action of which involves acceleration of oxidation, thus leading to post-irradiation regrowth of tumor. 6 For the radiation therapy of hypoxic tumor cells, there have been various strategies including hyperbaric oxygen therapy, 7,8 hypoxic cell radiosensitizers, [9][10][11][12] and hypoxic cytotoxins. 13 A new strategy to overcome tumor hypoxia focuses on the combination of radiotherapy and chemotherapy into prodrugs that are activated to release antitumor agents by hypoxic irradiation.…”
mentioning
confidence: 99%
“…[1][2][3][4][5] Hypoxic cells have been recognized to show resistance to ionizing radiation, the biological action of which involves acceleration of oxidation, thus leading to post-irradiation regrowth of tumor. 6 For the radiation therapy of hypoxic tumor cells, there have been various strategies including hyperbaric oxygen therapy, 7,8 hypoxic cell radiosensitizers, [9][10][11][12] and hypoxic cytotoxins. 13 A new strategy to overcome tumor hypoxia focuses on the combination of radiotherapy and chemotherapy into prodrugs that are activated to release antitumor agents by hypoxic irradiation.…”
mentioning
confidence: 99%
“…41 It is therefore likely that depletion of GSH in tumor cells is an effective target for radiation therapy. We have proposed a series of nitroazole radiosensitizers containing an a,b-unsaturated carbonyl group ( 22) 42 or propargylic sulfones ( 23) 43 in the side chains, which are able to capture GSH in tumor cells by alkylation (Fig. 6).…”
Section: Nitroazole Radiosensitizers For Hypoxic Cancer Cell Treatmen...mentioning
confidence: 99%
“…These include metronidazole [3], misonidazole [4] (Fig. 1), and more recently bifunctional 2-nitroimidazole derivatives, possessing alkylating functionality, capable of anti-angiogenic activity [5] or depletion of endogenous non-protein thiols (NPSH) such as reduced glutathione [6]. These effects have been found to play a crucial function in determining the response of cells to several types of radiation.…”
Section: Introductionmentioning
confidence: 99%