Cell permeability as a parameter for lead generation in the protein Tyrosine kinase inhibition field

Based on the inverse relationship between polar surface area and cell permeability and capitalizing on the properties of pyrrolopyrimidines 1 as protein tyrosine kinase inhibitors, pyrrolopyridones 2 were designed and synthesized as potential leads for the development of novel inhibitors with improv...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-06, Vol.11 (12), p.1549-1552
Hauptverfasser: Papageorgiou, Christos, Camenisch, Gian, Borer, Xaver
Format: Artikel
Sprache:eng
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Zusammenfassung:Based on the inverse relationship between polar surface area and cell permeability and capitalizing on the properties of pyrrolopyrimidines 1 as protein tyrosine kinase inhibitors, pyrrolopyridones 2 were designed and synthesized as potential leads for the development of novel inhibitors with improved cell permeability properties. Capitalizing on the properties of the protein tyrosine kinase inhibitors 1, pyrrolopyridones 2 were designed and synthesized as potential leads for the development of novel compounds with improved cell permeability properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00022-1