title: Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
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.
authors.affiliation: Novartis Pharma AG, Therapeutic Areas Arthritis & Bone Metabolism, Basel, Switzerland. martin.missbach@pharma.novartis.com
authors.forename: M
authors.initials: M
authors.lastname: Missbach
authors.forename: E
authors.initials: E
authors.lastname: Altmann
authors.forename: L
authors.initials: L
authors.lastname: Widler
authors.forename: M
authors.initials: M
authors.lastname: Susa
authors.forename: E
authors.initials: E
authors.lastname: Buchdunger
authors.forename: H
authors.initials: H
authors.lastname: Mett
authors.forename: T
authors.initials: T
authors.lastname: Meyer
authors.forename: J
authors.initials: J
authors.lastname: Green
mesh_terms: D000818:Animals; D015153:Blotting, Western; D000081247:CSK Tyrosine-Protein Kinase; D002645:Chickens; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D010766:Phosphorylation; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D019061:src-Family Kinases
chemical_list: D004791:Enzyme Inhibitors; D011743:Pyrimidines; D011758:Pyrroles; D011505:Protein-Tyrosine Kinases; D000081247:CSK Tyrosine-Protein Kinase; D019061:src-Family Kinases