Design, Synthesis and Anticancer Evaluation of Nitroimidazole Radiosensitisers

Autor: Hay, Lydia P. Liew, Avik Shome, Way W. Wong, Cho R. Hong, Kevin O. Hicks, Stephen M. F. Jamieson, Michael P.
Jazyk: angličtina
Rok vydání: 2023
Předmět:
Zdroj: Molecules; Volume 28; Issue 11; Pages: 4457
ISSN: 1420-3049
DOI: 10.3390/molecules28114457
Popis: The role of hypoxic tumour cells in resistance to radiotherapy, and in suppression of immune response, continues to endorse tumour hypoxia as a bona fide, yet largely untapped, drug target. Radiotherapy innovations such as stereotactic body radiotherapy herald new opportunities for classical oxygen-mimetic radiosensitisers. Only nimorazole is used clinically as a radiosensitiser, and there is a dearth of new radiosensitisers in development. In this report, we augment previous work to present new nitroimidazole alkylsulfonamides and we document their cytotoxicity and ability to radiosensitise anoxic tumour cells in vitro. We compare radiosensitisation with etanidazole and earlier nitroimidazole sulfonamide analogues and we identify 2-nitroimidazole and 5-nitroimidazole analogues with marked tumour radiosensitisation in ex vivo assays of surviving clonogens and with in vivo tumour growth inhibition.
Databáze: OpenAIRE
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