THE DEVELOPMENT OF NOVEL PHOTOSWITCHABLE KINASE INHIBITORS

Información del proyecto

RET PHOTOSWITCH

Identificador del acuerdo de subvención: 797049

DOI

10.3030/797049

Proyecto cerrado

Fecha de la firma de la CE 4 Abril 2018

Fecha de inicio 1 Octubre 2018

Fecha de finalización 30 Septiembre 2020

Financiado con arreglo a

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Coste total

€ 185 857,20

Aportación de la UE

€ 185 857,20

Coordinado por

GOETEBORGS UNIVERSITET
Sweden

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

Período documentado: 2018-10-01 hasta 2020-09-30

Resumen del contexto y de los objetivos generales del proyecto

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.

Trabajo realizado desde el comienzo del proyecto hasta el final del período abarcado por el informe y los principales resultados hasta la fecha

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.

Avances que van más allá del estado de la técnica e impacto potencial esperado (incluida la repercusión socioeconómica y las implicaciones sociales más amplias del proyecto hasta la fecha)

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