THE DEVELOPMENT OF NOVEL PHOTOSWITCHABLE KINASE INHIBITORS

Project Information

RET PHOTOSWITCH

Grant agreement ID: 797049

DOI

10.3030/797049

Project closed

EC signature date 4 April 2018

Start date 1 October 2018

End date 30 September 2020

Funded under

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Total cost

€ 185 857,20

EU contribution

€ 185 857,20

Coordinated by

GOETEBORGS UNIVERSITET
Sweden

Periodic Reporting for period 1 - RET PHOTOSWITCH (THE DEVELOPMENT OF NOVEL PHOTOSWITCHABLE KINASE INHIBITORS)

Reporting period: 2018-10-01 to 2020-09-30

Summary of the context and overall objectives of the project

The overall goal of the project was to develop novel photoswitchable RET kinase inhibitors (PKIs) with significant inhibitory activity difference between the two photoisomeric forms (E- and Z-isomers). The photochromic and thermal behaviour in water, the biological activity in biochemical, whole cell assays, as well as in zebrafish was to be evaluated. This project has achieved some of the objectives. We believe that the results generated from this project will appeal to a broad range of researchers from those working in the field of medicinal chemistry – switching drugs “on” and “off” with light to those interested in studying kinase inhibition, drug development and photo-pharmacology.

Work performed from the beginning of the project to the end of the period covered by the report and main results achieved so far

A manuscript of demonstrating the organic synthesis and photo-physical characterisations of novel PKIs is currently under preparation. The photo-controlled biochemical assay testing of PKIs are currently ongoing.

Progress beyond the state of the art and expected potential impact (including the socio-economic impact and the wider societal implications of the project so far)

switching drugs “on” and “off” with light are useful in studying kinase inhibition, drug development and photo-pharmacology.

Synthesis of pyrazolo(1,5a)-pyrimidine RET kinase inhibitor