Structural simplification of bioactive natural products with multicomponent synthesis: dihydropyridopyrazole analogues of podophyllotoxin
| Autor: | Nikolai M. Przheval’skii, Alexander Kornienko, Scott T. Shors, Elena A. Rozhkova, Severine Van slambrouck, Wim F.A. Steelant, Madhuri Manpadi, Snezna Rogelj, Igor V. Magedov |
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| Rok vydání: | 2006 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Antineoplastic Agents Apoptosis Jurkat cells Biochemistry Chemical synthesis Article chemistry.chemical_compound Jurkat Cells Structure-Activity Relationship Drug Discovery medicine Methods Organic chemistry Structure–activity relationship Humans Cytotoxicity Molecular Biology Podophyllotoxin Lignan chemistry.chemical_classification Biological Products Natural product Organic Chemistry General Medicine Combinatorial chemistry chemistry Molecular Medicine Pyrazoles Tetronic acid Lactone medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 17(5) |
| ISSN: | 0960-894X |
| Popis: | A three-component condensation of 5-amino-3-methylpyrazole, tetronic acid, and various aromatic, heteroaromatic, and aliphatic aldehydes leads to the formation of dihydropyridopyrazole analogues of a cytotoxic lignan podophyllotoxin. This new heterocyclic scaffold-based library allows a drastic reduction of the structural complexity of the natural product with the retention of its potent cytotoxic properties. Similarly to podophyllotoxin, the presented analogues induce apoptosis in Jurkat cells. |
| Databáze: | OpenAIRE |
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