Synthesis and activity of staurosporine analogs with a lactone functionality
| Autor: | Toshiaki Sunazuka, Li Zhuorong, Nobuyuki Funato, Koichiro Fukuda, Minoru Seto, Yoshihiro Harigaya, Satoshi Ōmura, Mieko Iguchi, Yasuharu Sasaki, Rintaro Yamada, Yutaka Ohmori, Yuzuru Iwai, Makoto Nasu, Masashi Kawanishi |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
chemistry.chemical_classification
Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Intramolecular cyclization Pharmaceutical Science Smooth muscle contraction Biochemistry Combinatorial chemistry Drug Discovery medicine Molecular Medicine Staurosporine Selectivity Molecular Biology Lactone medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 6:1893-1896 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/0960-894x(96)00343-5 |
| Popis: | Staurosporine analogs, whose γ-lactam functionality was converted into γ-lactone, were synthesized. The key step involves remarkably efficient ring-opening and then intramolecular cyclization reactions. In general, those compounds display potent anti-platelet aggregation activity and show higher selectivity against platelet as compared with smooth muscle contraction. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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