jm7b01678_si_002.csv (3.21 kB)
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides
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posted on 2017-12-18, 00:00 authored by Muriel Bonnet, Cho Rong Hong, Way Wua Wong, Lydia P. Liew, Avik Shome, Jingli Wang, Yongchuan Gu, Ralph J. Stevenson, Wen Qi, Robert F. Anderson, Frederik B. Pruijn, William R. Wilson, Stephen M. F. Jamieson, Kevin O. Hicks, Michael P. HayInnovations 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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Keywords
oxygen-mimetic radiosensitizerstumor hypoxiavivo assaysstereotactic body radiotherapytumor regrowth delaynovel nitroimidazole alkylsulfonamidesphosphate prodrug approachNitroimidazole Alkylsulfonamides Innovationstumor radiosensitization5- nitroimidazole analogueradiosensitize anoxic tumor cellsNext-Generation Hypoxic Cell Radiosensitizerstumor drug deliveryhypoxic tumor cellsdrug target2- nitroimidazole
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