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Cell permeability as a parameter for lead generation in the protein Tyrosine kinase inhibition field
C Papageorgiou1, G Camenisch, X Borer
1Novartis Pharma AG, WSJ350.3.14, CH-4002 Basel, Switzerland. christos.papageorgiou@pharma.novartis.com
Bioorganic & Medicinal Chemistry Letters
|June 20, 2001
Abstract:
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.