Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck

David J Calderwood; David N Johnston; Rainer Munschauer; Paul Rafferty

doi:10.1016/s0960-894x(02)00195-6

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1683-6. doi: 10.1016/s0960-894x(02)00195-6.

Authors

David J Calderwood¹, David N Johnston, Rainer Munschauer, Paul Rafferty

Affiliation

¹ Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA. david.calderwood@abbott.com

PMID: 12039590
DOI: 10.1016/s0960-894x(02)00195-6

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.

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Humans
Jurkat Cells
Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / analysis*
Pyrimidines / chemistry*
Pyrimidines / pharmacology*

Substances

Enzyme Inhibitors
Pyrimidines
Lymphocyte Specific Protein Tyrosine Kinase p56(lck)