title: Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
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.
authors.affiliation: Abbott, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze@abbott.com
authors.forename: Irini
authors.initials: I
authors.lastname: Akritopoulou-Zanze
authors.forename: Daria
authors.initials: D
authors.lastname: Darczak
authors.forename: Kathy
authors.initials: K
authors.lastname: Sarris
authors.forename: Kathleen M
authors.initials: KM
authors.lastname: Phelan
authors.forename: Jeffrey R
authors.initials: JR
authors.lastname: Huth
authors.forename: Danying
authors.initials: D
authors.lastname: Song
authors.forename: Eric F
authors.initials: EF
authors.lastname: Johnson
authors.forename: Yong
authors.initials: Y
authors.lastname: Jia
authors.forename: Stevan W
authors.initials: SW
authors.lastname: Djuric
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D010770:Phosphotransferases / Q000737:chemistry*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D011720:Pyrazoles; D010770:Phosphotransferases; D040301:Vascular Endothelial Growth Factor Receptor-2