Studies on protein kinase C inhibitors; structure-activity relationships in indolocarbazole and bis-indole series.
To assess the role of the cyclic amide moiety in indolocarbazole and bis-indole protein kinase C inhibitors, five amides in these series were synthesized in which the amide group is acyclic. These new compounds have no inhibitory effect on protein kinase C, indicating that the rigid cyclic structure of the amide group is compulsory for biological activity.
Fabre
S
S
Université Blaise Pascal, Laboratoire de Chimie Organique Biologique, URA 485, Aubière, France.
Prudhomme
M
M
Rapp
M
M
D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017868:Cyclic AMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D002227:Carbazoles; D007211:Indoles; D017868:Cyclic AMP-Dependent Protein Kinases; D011493:Protein Kinase C