title: Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.
abstract: A series of pyrrolo[2,3-d]pyrimidines was synthesized and evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided compound 13, an orally available lck inhibitor which inhibited TCR mediated IL-2 production after oral dosing.
authors.affiliation: Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA. david.calderwood@abbott.com
authors.forename: David J
authors.initials: DJ
authors.lastname: Calderwood
authors.forename: David N
authors.initials: DN
authors.lastname: Johnston
authors.forename: Rainer
authors.initials: R
authors.lastname: Munschauer
authors.forename: Paul
authors.initials: P
authors.lastname: Rafferty
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D019169:Jurkat Cells; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000032:analysis*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D011743:Pyrimidines; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)