| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377743 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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.
Graphical abstract4-(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.Figure optionsDownload full-size imageDownload as PowerPoint slide
