THE DEVELOPMENT OF NOVEL PHOTOSWITCHABLE KINASE INHIBITORS

Informazioni relative al progetto

RET PHOTOSWITCH

ID dell’accordo di sovvenzione: 797049

DOI

10.3030/797049

Progetto chiuso

Data della firma CE 4 Aprile 2018

Data di avvio 1 Ottobre 2018

Data di completamento 30 Settembre 2020

Finanziato da

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Costo totale

€ 185 857,20

Contributo UE

€ 185 857,20

Coordinato da

GOETEBORGS UNIVERSITET
Sweden

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

Periodo di rendicontazione: 2018-10-01 al 2020-09-30

Sintesi del contesto e degli obiettivi generali del progetto

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.

Lavoro eseguito dall’inizio del progetto fino alla fine del periodo coperto dalla relazione e principali risultati finora ottenuti

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.

Progressi oltre lo stato dell’arte e potenziale impatto previsto (incluso l’impatto socioeconomico e le implicazioni sociali più ampie del progetto fino ad ora)

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