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. 2006 Sep 1;16(17):4686-91.
doi: 10.1016/j.bmcl.2006.05.090. Epub 2006 Jun 13.

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

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

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

Kimberly G Petrov et al. Bioorg Med Chem Lett. .

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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