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Bioorg Med Chem Lett. 2006 Sep 1;16(17):4686-91. Epub 2006 Jun 13.

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

Author information

1
GlaxoSmithKline, Research Triangle Park, NC, USA.

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.

PMID:
16777410
DOI:
10.1016/j.bmcl.2006.05.090
[Indexed for MEDLINE]

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