Lessons from (S)-6-(1-(6-(1-Methyl-1 H-pyrazol-4-yl)-[1, 2, 4] triazolo [4, 3-b] pyridazin-3-yl) ethyl) quinoline (PF-04254644), an Inhibitor of Receptor Tyrosine Kinase c- …

JJ Cui, H Shen, M Tran-Dubé, M Nambu…

Index: Cui, J. Jean; Shen, Hong; Tran-Dube, Michelle; Nambu, Mitchell; McTigue, Michele; Grodsky, Neil; Ryan, Kevin; Yamazaki, Shinji; Aguirre, Shirley; Parker, Max; Li, Qiuhua; Zou, Helen; Christensen, James Journal of Medicinal Chemistry, 2013 , vol. 56, # 17 p. 6651 - 6665

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Citation Number: 8

Abstract

The hepatocyte growth factor (HGF)/c-Met signaling axis is deregulated in many cancers and plays important roles in tumor invasive growth and metastasis. An exclusively selective c-Met inhibitor (S)-6-(1-(6-(1-methyl-1 H-pyrazol-4-yl)-[1, 2, 4] triazolo [4, 3-b] pyridazin-3-yl) ethyl) quinoline (8) was discovered from a highly selective high-throughput screening hit via structure-based drug design and medicinal chemistry lead optimization. Compound 8 had ...