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  • Title: Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
    Author: Bonnet M, Hong CR, Wong WW, Liew LP, Shome A, Wang J, Gu Y, Stevenson RJ, Qi W, Anderson RF, Pruijn FB, Wilson WR, Jamieson SMF, Hicks KO, Hay MP.
    Journal: J Med Chem; 2018 Feb 08; 61(3):1241-1254. PubMed ID: 29253343.
    Abstract:
    Innovations in the field of radiotherapy such as stereotactic body radiotherapy, along with the advent of radio-immuno-oncology, herald new opportunities for classical oxygen-mimetic radiosensitizers. The role of hypoxic tumor cells in resistance to radiotherapy and in suppression of immune response continues to endorse tumor hypoxia as a bona fide, yet largely untapped, drug target. Only nimorazole is used clinically as a radiosensitizer, and there is a dearth of new radiosensitizers in development. Here we present a survey of novel nitroimidazole alkylsulfonamides and document their cytotoxicity and ability to radiosensitize anoxic tumor cells in vitro. We use a phosphate prodrug approach to increase aqueous solubility and to improve tumor drug delivery. A 2-nitroimidazole and a 5-nitroimidazole analogue demonstrated marked tumor radiosensitization in either ex vivo assays of surviving clonogens or tumor regrowth delay.
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