Details

Autor(en) / Beteiligte

• 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.
• Hartman, George D.

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1146-1150

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2006

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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. 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.