Bioorganic and Medicinal Chemistry Letters p. 351 - 355 (2004)
Update date:2022-08-02
Topics:
Fraley, Mark E.
Arrington, Kenneth L.
Buser, Carolyn A.
Ciecko, Patrice A.
Coll, Kathleen E.
Fernandes, Christine
Hartman, George D.
Hoffman, William F.
Lynch, Joseph J.
McFall, Rosemary C.
Rickert, Keith
Singh, Romi
Smith, Sheri
Thomas, Kenneth A.
Wong, Bradley K.
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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