Title : Catalyst-free synthesis of quinazolin-4-ones from (hetero)aryl-guanidines: application to the synthesis of pyrazolo[4,3-f]quinazolin-9-ones, a new family of DYRK1A inhibitors.

Pub. Date : 2012 Nov

PMID : 22991074






1 Functional Relationships(s)
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1 The most active molecules, 7-(2-hydroxyethylamino)- and 7-(3-hydroxypropylamino)-pyrazolo[4,3-f]quinazolin-9-ones, inhibit DYRK1A and CLK1 at submicromolar concentrations, indicating the potential interest of this new heterocycle in drug design. 7-(3-hydroxypropylamino)-pyrazolo[4,3-f]quinazolin-9-ones CDC like kinase 1 Homo sapiens