Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
Publication
, Journal Article
Petrov, KG; Zhang, Y-M; Carter, M; Cockerill, GS; Dickerson, S; Gauthier, CA; Guo, Y; Mook, RA; Rusnak, DW; Walker, AL; Wood, ER; Lackey, KE
Published in: Bioorg Med Chem Lett
September 1, 2006
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.
Duke Scholars
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Published In
Bioorg Med Chem Lett
DOI
ISSN
0960-894X
Publication Date
September 1, 2006
Volume
16
Issue
17
Start / End Page
4686 / 4691
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Receptor, erbB-2
- Receptor, ErbB-2
- Quinazolines
- Protein Kinase Inhibitors
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Lapatinib
- Inhibitory Concentration 50
Citation
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Petrov, K. G., Zhang, Y.-M., Carter, M., Cockerill, G. S., Dickerson, S., Gauthier, C. A., … Lackey, K. E. (2006). Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. Bioorg Med Chem Lett, 16(17), 4686–4691. https://doi.org/10.1016/j.bmcl.2006.05.090
Petrov, Kimberly G., Yue-Mei Zhang, Malcolm Carter, G Stuart Cockerill, Scott Dickerson, Cassandra A. Gauthier, Yu Guo, et al. “Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.” Bioorg Med Chem Lett 16, no. 17 (September 1, 2006): 4686–91. https://doi.org/10.1016/j.bmcl.2006.05.090.
Petrov KG, Zhang Y-M, Carter M, Cockerill GS, Dickerson S, Gauthier CA, et al. 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.
Petrov, Kimberly G., et al. “Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.” Bioorg Med Chem Lett, vol. 16, no. 17, Sept. 2006, pp. 4686–91. Pubmed, doi:10.1016/j.bmcl.2006.05.090.
Petrov KG, Zhang Y-M, Carter M, Cockerill GS, Dickerson S, Gauthier CA, Guo Y, Mook RA, Rusnak DW, Walker AL, Wood ER, Lackey KE. 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):4686–4691.
Published In
Bioorg Med Chem Lett
DOI
ISSN
0960-894X
Publication Date
September 1, 2006
Volume
16
Issue
17
Start / End Page
4686 / 4691
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Receptor, erbB-2
- Receptor, ErbB-2
- Quinazolines
- Protein Kinase Inhibitors
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Lapatinib
- Inhibitory Concentration 50