1458639-33-2

Upstream product

• 20197-55-1 6,8-dichloro-2H-[1,3]dioxolo[4,5-g]quinazoline 
• 187164-87-0 5-amino-6-cyanobenzo<1,3>dioxale 
• 52805-38-6 6-nitro-1,3-benzodioxole-5-carbonitrile 
• 4421-09-4 piperonylonitrile 
• 110-89-4 piperidine 
• 1458639-52-5 C₂₁H₂₁ClN₄O₂ 

Relevant academic research and scientific papers

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

G9a is a histone lysine methyltransferase (HKMT) involved in epigenetic regulation via the installation of histone methylation marks. 6,7-Dimethoxyquinazoline analogues, such as BIX-01294, are established as potent, substrate competitive inhibitors of G9a. With an objective to identify novel chemotypes for substrate competitive inhibitors of G9a, we have designed and synthesised a range of heterocyclic scaffolds, and investigated their ability to inhibit G9a. These studies have led to improved understanding of the key pharmacophoric features of BIX-01294 and the identification of a new core quinoline inhibitory scaffold, which retains excellent potency and high selectivity. Molecular docking was carried out to explain the observed in vitro data. This journal is

QUINAZOLINE COMPOUNDS AND THEIR USE IN THERAPY

This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.