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Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.

Authors
  • Sisko, John T
  • Tucker, Thomas J
  • Bilodeau, Mark T
  • Buser, Carolyn A
  • Ciecko, Patrice A
  • Coll, Kathleen E
  • Fernandes, Christine
  • Gibbs, Jackson B
  • Koester, Timothy J
  • Kohl, Nancy
  • Lynch, Joseph J
  • Mao, Xianzhi
  • McLoughlin, Debra
  • Miller-Stein, Cynthia M
  • Rodman, Leonard D
  • Rickert, Keith W
  • Sepp-Lorenzino, Laura
  • Shipman, Jennifer M
  • Thomas, Kenneth A
  • Wong, Bradley K
  • And 1 more
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Mar 01, 2006
Volume
16
Issue
5
Pages
1146–1150
Identifiers
PMID: 16368234
Source
Medline
License
Unknown

Abstract

Pyrimidino-thiazolyl carbonitriles were prepared that are potent VEGFR-2 (KDR) kinase inhibitors. The modification of lead structures resulted in 3m which exhibited the best overall profile in KDR inhibitory activity, iv/po pharmacokinetics, and reduced hERG affinity.

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