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Synfacts 2021; 17(09): 1043
DOI: 10.1055/s-0040-1720783
Chemistry in Medicine and Biology

X-ray Irradiation Promoted Activation of Prodrugs

Contributor(s):
Dirk Trauner
,
Zisis Peitsinis
Geng J, *, Zhang Y, Gao Q, Neumann K, Dong H, Porter H, Potter M, Ren H, Argyle D, Bradley M. * University of Edinburgh, UK and the Shenzhen Institute of Advanced Technology, P. R. of China
Switching on Prodrugs Using Radiotherapy.

Nat. Chem. 2021;
13: 805-810
DOI: 10.1038/s41557-021-00711-4.
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Key words

cancer prodrugs - radiotherapy - X-ray irradiation

Significance

Activating an anticancer prodrug with clinical doses of ionizing radiation could enable localized release of a drug at the tumor site and potentially eliminate the global systemic toxicity of conventional chemo-radiotherapy. In a tumor-bearing mice model, the combination of caged prodrug and X-ray treatment not only inhibited tumor growth but also reduced doxorubicin-induced heart toxicity.


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Comment

The caged doxorubicin prodrug was synthesized in two steps, by following a reported procedure (Bioconjugate Chem. 2018, 29, 324). Decaging of doxorubicin was achieved using X-ray irradiation (from 0 to 60 Gy) through radical reduction of the tetrafluorophenyl azide followed by 1,6-self-immolation linker cleavage.


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Publication History

Article published online:
18 August 2021

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