A facile access to novel steroidal 17-2′-(1′,3′,4′)-oxadiazoles, and an evaluation of their cytotoxic activities in vitro
| Autor: | Ida Kovács, János Wölfling, Gergő Mótyán, Éva Frank, Dóra Kovács, István Zupkó |
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| Rok vydání: | 2014 |
| Předmět: |
Cell Survival
Stereochemistry medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Aldehyde Steroid HeLa Cell Line Tumor Drug Discovery medicine Humans Potency Moiety Cytotoxic T cell Microwaves Molecular Biology chemistry.chemical_classification Cisplatin Oxadiazoles biology Organic Chemistry biology.organism_classification In vitro Sterols chemistry Molecular Medicine Oxidation-Reduction HeLa Cells medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 24:1265-1268 |
| ISSN: | 0960-894X |
| Popis: | Novel types of 17- exo -heterocycles in the Δ 5 androstene series carrying an 1,3,4-oxadiazole moiety were efficiently synthesized via aldehyde N -acylhydrazone intermediates, obtained from the microwave-assisted condensation of 3β-hydroxy- or 3β-acetoxyandrost-5-ene-17β-carbaldehyde with different acylhydrazides. The subsequent phenyl iodonium diacetate-induced oxidative cyclization proceeded under mild conditions. The synthesized compounds were subjected to in vitro pharmacological studies to investigate their antiproliferative activities on four malignant adherent cell lines (HeLa, MCF7, A2780 and A431), and exhibited the highest potency against HeLa cells, some of them revealing action comparable to that of the reference agent cisplatin. |
| Databáze: | OpenAIRE |
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