Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
We report the synthesis of kinase targeted libraries based on the thienopyrazole scaffold. Several thienopyrazole analogs have been identified as submicromolar inhibitors of KDR.
Akritopoulou-Zanze
Irini
I
Abbott, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze@abbott.com
Darczak
Daria
D
Sarris
Kathy
K
Phelan
Kathleen M
KM
Huth
Jeffrey R
JR
Song
Danying
D
Johnson
Eric F
EF
Jia
Yong
Y
Djuric
Stevan W
SW
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*
D004791:Enzyme Inhibitors; D011720:Pyrazoles; D010770:Phosphotransferases; D040301:Vascular Endothelial Growth Factor Receptor-2