Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 3, Pages 1241-1254Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01678
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Funding
- Australian Institute for Nuclear Sciences and Engineering
- University of Auckland's Biopharma Thematic Research Initiative
- UniServices Investment/Ministry of Business, Innovation and Employment Pre Seed Accelerator Fund
- Cancer Society of New Zealand [14/17]
- Health Research Council of NZ [16/120]
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Innovations in the field of radiotherapy such as stereotactic body radiotherapy, along with the advent of radio-N 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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