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. 2000 Oct 2;10(19):2171-4.
doi: 10.1016/s0960-894x(00)00442-x.

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

A F Burchat  1 , D J Calderwood, G C Hirst, N J Holman, D N Johnston, R Munschauer, P Rafferty, G B Tometzki
Affiliations

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

A F Burchat et al. Bioorg Med Chem Lett. .

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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