Phosphate linkers with traceable cyclic intermediates for self-immolation detection and monitoring

0539202 - ÚOCHB 2022 RIV GB eng J - Journal Article
Procházková, Eliška - Šimon, P. - Straka, Michal - Filo, J. - Májek, M. - Cigáň, M. - Baszczyňski, O.
Phosphate linkers with traceable cyclic intermediates for self-immolation detection and monitoring.
Chemical Communications. Roč. 57, č. 2 (2021), s. 211-214. ISSN 1359-7345. E-ISSN 1364-548X
Institutional support: RVO:61388963
Keywords : protecting groups * pKa values * phenols
OECD category: Analytical chemistry
Impact factor: 6.065, year: 2021
Method of publishing: Limited access
https://doi.org/10.1039/D0CC06928K

Self-immolation (SI) is the key principle of ProTide nucleotide prodrugs such as remdesivir, which is currently used to treat COVID-19 patients. Developing novel tailor-made SI systems requires new analytical methods for the detection and monitoring of SI. We developed a robust method for SI analysis using novel phosphate-based SI linkers with NMR traceable cyclic intermediates to distinguish SI from alternative fragmentation pathways and to monitor cargo release in real time.
Permanent Link: http://hdl.handle.net/11104/0317236