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THE DEVELOPMENT OF NOVEL PHOTOSWITCHABLE KINASE INHIBITORS

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

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

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.
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.
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