Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors

Irini Akritopoulou-Zanze; Daria Darczak; Kathy Sarris; Kathleen M Phelan; Jeffrey R Huth; Danying Song; Eric F Johnson; Yong Jia; Stevan W Djuric

doi:10.1016/j.bmcl.2005.09.042

Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors

Bioorg Med Chem Lett. 2006 Jan 1;16(1):96-9. doi: 10.1016/j.bmcl.2005.09.042. Epub 2005 Oct 10.

Authors

Irini Akritopoulou-Zanze¹, Daria Darczak, Kathy Sarris, Kathleen M Phelan, Jeffrey R Huth, Danying Song, Eric F Johnson, Yong Jia, Stevan W Djuric

Affiliation

¹ Abbott, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze@abbott.com

PMID: 16216502
DOI: 10.1016/j.bmcl.2005.09.042

Abstract

We report the synthesis of kinase targeted libraries based on the thienopyrazole scaffold. Several thienopyrazole analogs have been identified as submicromolar inhibitors of KDR.

MeSH terms

Chemistry, Pharmaceutical / methods*
Drug Design*
Drug Evaluation, Preclinical
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Humans
Inhibitory Concentration 50
Models, Chemical
Phosphotransferases / chemistry*
Pyrazoles / chemical synthesis*
Pyrazoles / chemistry*
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*
Vascular Endothelial Growth Factor Receptor-2 / chemistry*

Substances

Enzyme Inhibitors
Pyrazoles
Phosphotransferases
Vascular Endothelial Growth Factor Receptor-2