N-(carbacyclyl)-indolocarbazoles, such as I [R = substituted or unsubstituted 5 or 6 membered carbacyclyl; R3, R4 = H, halogen, alkyl, carboxy, carboxamide, amino, alkoxy, etc.], were prepd. as protein kinase inhibitors which are useful for the treatment of non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, malignant diseases, and neurodegenerative diseases, such as Alzheimer's disease. Thus, NAD 006 (II) was prepd. via a multistep synthetic sequence starting from cyclopentadiene, 1H-indole-3-acetonitrile and 2-indolone. The prepd. staurosporine analogs were assayed for inhibition of extracellular signal regulated kinase 2, protein kinase A, protein kinase C and glycogen synthase kinase 3β.
Preparation of N-carbacycle monosubstituted indolocarbazoles for therapeutic use as protein kinase inhibitors / H. Sahagun Krause, O. Thillaye Du Boullay, V. Thillaye Du Boullay, L. Casiraghi, P. Seneci, H. Klafki, T. Braxmeier, S. Mueller, W. Froehner, B. Monse, S. Gordon, H. Roder.
Preparation of N-carbacycle monosubstituted indolocarbazoles for therapeutic use as protein kinase inhibitors
P. Seneci;
2003
Abstract
N-(carbacyclyl)-indolocarbazoles, such as I [R = substituted or unsubstituted 5 or 6 membered carbacyclyl; R3, R4 = H, halogen, alkyl, carboxy, carboxamide, amino, alkoxy, etc.], were prepd. as protein kinase inhibitors which are useful for the treatment of non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, malignant diseases, and neurodegenerative diseases, such as Alzheimer's disease. Thus, NAD 006 (II) was prepd. via a multistep synthetic sequence starting from cyclopentadiene, 1H-indole-3-acetonitrile and 2-indolone. The prepd. staurosporine analogs were assayed for inhibition of extracellular signal regulated kinase 2, protein kinase A, protein kinase C and glycogen synthase kinase 3β.
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