Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src

M Missbach; E Altmann; L Widler; M Susa; E Buchdunger; H Mett; T Meyer; J Green

doi:10.1016/s0960-894x(00)00131-1

Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src

Bioorg Med Chem Lett. 2000 May 1;10(9):945-9. doi: 10.1016/s0960-894x(00)00131-1.

Authors

M Missbach¹, E Altmann, L Widler, M Susa, E Buchdunger, H Mett, T Meyer, J Green

Affiliation

¹ Novartis Pharma AG, Therapeutic Areas Arthritis & Bone Metabolism, Basel, Switzerland. martin.missbach@pharma.novartis.com

PMID: 10853665
DOI: 10.1016/s0960-894x(00)00131-1

Abstract

5,7-Diphenyl-pyrrolo[2,3d]pyrimidines represent a new class of highly potent inhibitors of the tyrosine kinase c-Src (IC50 < 50 nM) with specificity against a panel of different tyrosine kinases. The substitution pattern on the two phenyl rings determines potency and specificity and provides a means to modulate cellular activity.

MeSH terms

Animals
Blotting, Western
CSK Tyrosine-Protein Kinase
Chickens
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Models, Molecular
Phosphorylation
Protein-Tyrosine Kinases / antagonists & inhibitors*
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology
Pyrroles / chemical synthesis*
Pyrroles / pharmacology
Structure-Activity Relationship
Substrate Specificity
src-Family Kinases

Substances

Enzyme Inhibitors
Pyrimidines
Pyrroles
Protein-Tyrosine Kinases
CSK Tyrosine-Protein Kinase
src-Family Kinases