2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2305-9. doi: 10.1016/j.bmcl.2007.01.057.
Erin F DiMauro 1,  John Newcomb,  Joseph J Nunes,  Jean E Bemis,  Christina Boucher,  John L Buchanan,  William H Buckner,  Alan Cheng,  Theodore Faust,  Faye Hsieh,  Xin Huang,  Josie H Lee,  Teresa L Marshall,  Matthew W Martin,  David C McGowan,  Stephen Schneider,  Susan M Turci,  Ryan D White,  Xiaotian Zhu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. [email protected]
PMID: 17280833 DOI: 10.1016/j.bmcl.2007.01.057
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.

Figures