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Bioorg Med Chem Lett. 2007 Apr 15;17(8):2305-9. Epub 2007 Jan 25.

Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.

Author information

1
Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. edimauro@amgen.com

Erratum in

  • Bioorg Med Chem Lett. 2007 Sep 15;17(18):5280.

Abstract

4-Amino-5,6-biaryl-furo[2,3-d]pyrimidines were identified as potent non-selective inhibitors of Lck. A novel, divergent, and practical synthetic route was developed to access derivatives from bifunctional intermediates. Lead optimization was guided by X-ray crystallographic data, and preliminary SAR led to the identification of compounds with improved cellular potency and selectivity.

PMID:
17280833
DOI:
10.1016/j.bmcl.2007.01.057
[Indexed for MEDLINE]

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