Referenced in: none

Automatically associated channels: Kv11.1

Title: Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.

Authors: 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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2004 Jan 19 , 14, 351-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/14698157

Abstract
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 I(Kr) potassium channel hERG.