Synthesis of novel 5-substituted indirubins as protein kinases inhibitors.
In an effort to identify new pharmacological inhibitors of disease-relevant protein kinases with increased potency and selectivity, we synthesized and evaluated new 5-substituted indirubins. The effects of 34 indirubin derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3, as well as on SH-SY5Y human neuroblastoma cell survival, were investigated.
Beauchard
Anne
A
Laboratoire de Biotechnologies et de Chimie Bio-organique, FRE CNRS 2766, UFR Sciences Fondamentales et Sciences pour l'Ingénieur, Université de La Rochelle, Bâtiment Marie Curie, 17042 La Rochelle, France.
Ferandin
Yoan
Y
Frère
Stéphane
S
Lozach
Olivier
O
Blairvacq
Mélina
M
Meijer
Laurent
L
Thiéry
Valérie
V
Besson
Thierry
T
D000818:Animals; D042846:CDC2-CDC28 Kinases / Q000037:antagonists & inhibitors*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D008970:Molecular Weight; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013215:Starfish; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013552:Swine
D007211:Indoles; D047428:Protein Kinase Inhibitors; D042846:CDC2-CDC28 Kinases; D038362:Glycogen Synthase Kinase 3; C027185:indirubin