2. Academic Validation
  3. Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4686-91. doi: 10.1016/j.bmcl.2006.05.090.
Kimberly G Petrov 1,  Yue-Mei Zhang,  Malcolm Carter,  G Stuart Cockerill,  Scott Dickerson,  Cassandra A Gauthier,  Yu Guo,  Robert A Mook Jr,  David W Rusnak,  Ann L Walker,  Edgar R Wood,  Karen E Lackey
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Research Triangle Park, NC, USA.
PMID: 16777410 DOI: 10.1016/j.bmcl.2006.05.090
Abstract

Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best Enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the Enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.

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