Synthesis and biological evaluation of (+)-neopeltolide analogues: Importance of the oxazole-containing side chain
| Autor: | Masato Kawakami, Makoto Sasaki, Haruhiko Fuwa, Takuma Noguchi |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Double bond
Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Neopeltolide Biochemistry Human lung Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery Side chain medicine Humans Pancreatic carcinoma Oxazoles Molecular Biology Cell Proliferation Biological evaluation Oxazole chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Organic Chemistry Stereoisomerism Methyl carbamate medicine.anatomical_structure chemistry Molecular Medicine Macrolides Drug Screening Assays Antitumor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 24:2415-2419 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2014.04.031 |
| Popis: | We describe the synthesis and biological evaluation of (+)-neopeltolide analogues with structural modifications in the oxazole-containing side chain. Evaluation of the antiproliferative activity of newly synthesized analogues against A549 human lung adenocarcinoma cells and PANC-1 human pancreatic carcinoma cells have shown that the C19-C20 and C26-C27 double bonds within the oxazole-containing side chain and the terminal methyl carbamate group are essential for potent activity. |
| Databáze: | OpenAIRE |
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