Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain
| Autor: | Sandra E. Wilkinson, Janet L. Smith, Peter D. Davis, Harris William, David R. Vesey, John S. Nixon, Geoffrey Lawton, Christopher H. Hill, Trevor J. Hallam |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
chemistry.chemical_classification
Bisindolylmaleimide biology Tertiary amine Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry chemistry.chemical_compound Enzyme Enzyme inhibitor Drug Discovery biology.protein Side chain Molecular Medicine Pharmacophore Binding site Molecular Biology Protein kinase C |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:1303-1308 |
| ISSN: | 0960-894X |
| Popis: | A pharmacophore model for the localisation of the cationic binding site of bisindolylmaleimide PKC inhibitors is described. This model has been used to guide selection of further conformationally restricted tertiary amine analogues, culminating in the identification and synthesis of the potent and highly selective PKC inhibitor, Ro 32-0557. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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