Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors

Mark E. Fraley,Kenneth L. Arrington,Carolyn A. Buser,Patrice A. Ciecko,Kathleen E. Coll,Christine Fernandes,George D. Hartman,William F. Hoffman,Joseph J. Lynch,Rosemary C. McFall,Keith Rickert,Romi Singh,Sheri Smith,Kenneth A. Thomas,Bradley K. Wong

Bioorganic & Medicinal Chemistry Letters（2004）

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摘要

Modifications to the basic side-chain of early lead structures of the indolyl quinolinone class of KDR kinase inhibitors resulted in improved pharmacokinetic and ancillary profiles. Specifically, compounds bearing 5-amido- and 5-sulphonamido-indolyl substituents exhibited lower plasma clearance and weaker binding affinity for the IKr potassium channel hERG. ©2003 Elsevier Science Ltd. All rights reserved.

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binding affinity,potassium channel

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