Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Amgen, Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA.

Published: September 2008

A novel class of potent and selective inhibitors of KDR incorporating an indazole moiety 1 is reported. The discovery, synthesis, and structure-activity relationships of this series of inhibitors have been investigated. The most promising compounds were also profiled to determine their pharmacokinetic properties and evaluated in a VEGF-induced vascular permeability assay.

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http://dx.doi.org/10.1016/j.bmcl.2008.07.080DOI Listing

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