A novel series of potent and selective IKK2 inhibitors

Alistair H Bingham; Richard J Davenport; Lewis Gowers; Roland L Knight; Christopher Lowe; David A Owen; David M Parry; Will R Pitt

doi:10.1016/j.bmcl.2003.10.047

A novel series of potent and selective IKK2 inhibitors

Bioorg Med Chem Lett. 2004 Jan 19;14(2):409-12. doi: 10.1016/j.bmcl.2003.10.047.

Authors

Alistair H Bingham¹, Richard J Davenport, Lewis Gowers, Roland L Knight, Christopher Lowe, David A Owen, David M Parry, Will R Pitt

Affiliation

¹ Celltech R&D Ltd, Granta Park, Great Abington, CB16GS, Cambridge, UK.

PMID: 14698170
DOI: 10.1016/j.bmcl.2003.10.047

Abstract

A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling.

MeSH terms

Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
I-kappa B Kinase
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / metabolism*
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology

Substances

Enzyme Inhibitors
Pyrimidines
Protein Serine-Threonine Kinases
I-kappa B Kinase