1036745-17-1Relevant academic research and scientific papers
Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors
Monastyrskyi, Andrii,Bayle, Simon,Quereda, Victor,Grant, Wayne,Cameron, Michael,Duckett, Derek,Roush, William
, p. 400 - 404 (2018)
The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 and 23, with submicromolar inhibitory activities against ASK1. Kinetic analysis demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described herein are ATP competitive.
