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Molecules 2016, 21(5), 570;

Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors

Institute of Pharmacy, University of Kiel, Gutenbergstr. 76, D-24118 Kiel, Germany
Author to whom correspondence should be addressed.
Academic Editor: Wiktor Szymański
Received: 16 March 2016 / Revised: 20 April 2016 / Accepted: 21 April 2016 / Published: 29 April 2016
(This article belongs to the Special Issue Photoresponsive Drugs)
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In this study, we report on the design, synthesis, photokinetic properties and in vitro evaluation of photoactivatable caged prodrugs for the receptor tyrosine kinase VEGFR-2. Highly potent VEGFR-2 inhibitors 1 and 3 were caged by introduction of a photoremovable protecting group (PPG) to yield the caged prodrugs 4 and 5. As expected, enzymatic and cellular proliferation assays showed dramatically diminished efficacy of caged prodrugs in vitro. Upon ultraviolet (UV) irradiation of the prodrugs original inhibitory activity was completely restored and even distinctly reinforced, as was the case for the prodrug 4. The presented results are a further evidence for caging technique being an interesting approach in the protein kinase field. It could enable spatial and temporal control for the inhibition of VEGFR-2. The described photoactivatable prodrugs might be highly useful as biological probes for studying the VEGFR-2 signal transduction. View Full-Text
Keywords: photoactivatable prodrugs; caging; receptor tyrosine kinase; kinase inhibitors; VEGFR-2; 3,4-diarylmaleimides; photoremovable protecting group (PPG) photoactivatable prodrugs; caging; receptor tyrosine kinase; kinase inhibitors; VEGFR-2; 3,4-diarylmaleimides; photoremovable protecting group (PPG)

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Pinchuk, B.; Horbert, R.; Döbber, A.; Kuhl, L.; Peifer, C. Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors. Molecules 2016, 21, 570.

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