ArticleChemistry (Weinheim an der Bergstrasse, Germany)2025
Oligoethylene Phosphoramidate-Based Kinase Inhibitor Prodrugs - Solubility, Enzyme Inhibition, and Hydrolysis.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
1 citing paper in PubMed.
- Oligoethylene Phosphoramidate-Based Kinase Inhibitor Prodrugs - Solubility, Enzyme Inhibition, and Hydrolysis.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
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Authors and funding
5 authors.
Funding
Abstract
The efficiency of kinase inhibiting cancer therapeutics is often limited by their poor solubility in water. PEGylation is one possible strategy to improve the solubility of the drug, however, means to cleave off the PEG after reaching the target is important to make use of the therapeutic effects of the native drug. Moreover, the length of the PEG chains will have an effect on the solubility and binding. In this study, we want to extend our understanding of solubilizing oligo ethylene glycol (OEG) chains connected to kinase inhibitors using a pH labile phosphoramidate linker. We synthesize a library of drug-OEG conjugates for Ceritinib, Crizotinib, Palbociclib, and Ribocilib kinase inhibitors with n=2, 3, 4 and 8 OEG repeat units. We study the influence on water solubility, enzyme inhibition, and pH induced hydrolysis. A maximum in solubility is obtained for n=3 or 4. We show that small differences in chain length can strongly influence the water solubility, while all other properties remain relatively comparable.
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