4.5 Article

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

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 17, 页码 4844-4848

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.07.080

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KDR inhibitor; VEGFR-2 inhibitor; kinase inhibitor

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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 pro. led to determine their pharmacokinetic properties and evaluated in a VEGF-induced vascular permeability assay. (C) 2008 Elsevier Ltd. All rights reserved.

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