Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

• DOI: 10.1039/c5md00210a
• Publication Date: 2015-08-11T08:02:19Z
• Authors: Richard J. R. Ell...; Ashley Jarvis; Mohan B. Rajasekaran; Malini Menon; Leandra Bowers; Ray Boffey; Melanie Bayford; Stuart Firth-Clark; Rebekah Key; Rehan Aqil; Stewart B. Kirton; Dan Niculescu-Duvaz; Laura Fish; Filipa Lopes; Robert McLeary; Ines Trindade; Elisenda Vendrell; Felix Munkonge; Rod Porter; Trevor Perrior; Caroline Springer; Antony W. Oliver; Laurence H. Pearl; Alan Ashworth; Christopher J. Lord
• Keywords: 0301 basic medicine; 03 medical and health sciences; ResearchInstitutes_Networks_Beacons/mcrc; name=Manchester Cancer Research Centre; 3. Good health

The tankyrase proteins (TNKS, TNKS2) are attractive anti-cancer drug targets, particularly as inhibition of their catalytic activity has been shown to antagonise oncogenic WNT signalling.