Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II

  • Bioorg Med Chem Lett. 2000 Oct 2;10(19):2171-4. doi: 10.1016/s0960-894x(00)00442-x.
A F Burchat  1 ,  D J Calderwood ,  G C Hirst ,  N J Holman ,  D N Johnston ,  R Munschauer ,  P Rafferty ,  G B Tometzki
Affiliations
  • 1. BASF Bioresearch Corporation, Worcester, MA 01605-5314, USA.
PMID: 11012022 DOI: 10.1016/s0960-894x(00)00442-x
Abstract

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are novel, potent and selective inhibitors of Lck in vitro. Exploration of C-6 position of the pyrrolo[2,3-d]pyrimidine and the terminal phenyl group structure-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models.

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