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

Authors
Burchat, AF Calderwood, DJ Hirst, GC Holman, NJ Johnston, DN Munschauer, R Rafferty, P Tometzki, GB
Citation
Af. Burchat et al., Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II, BIOORG MED, 10(19), 2000, pp. 2171-2174
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
19
Year of publication
2000
Pages
2171 - 2174
Database
ISI
SICI code
0960-894X(20001002)10:19<2171:PCAE5A>2.0.ZU;2-V
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 stru cture-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models. (C) 2000 Elsevier Science Ltd. All rights reserved.