Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.
We report the synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted kinase inhibitors. Initial efforts focused on the development of selective KDR inhibitors, while later strategies involved the improvement of potency toward multiple kinase targets. Thus, several compounds were identified as potent KDR, Flt1, Flt3, and c-Kit inhibitors.
Akritopoulou-Zanze
Irini
I
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze@abbott.com
Albert
Daniel H
DH
Bousquet
Peter F
PF
Cunha
George A
GA
Harris
Christopher M
CM
Moskey
Maria
M
Dinges
Jurgen
J
Stewart
Kent D
KD
Sowin
Thomas J
TJ
D000818:Animals; D006801:Humans; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*
D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D020794:Receptor Protein-Tyrosine Kinases