Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells
| Autor: | Jian Feng Zhan, Bin Hai Kuang, Jia Qi Wang, Qiao Li Lv, Guo Gang Tu, Shao-Hua Li |
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| Rok vydání: | 2014 |
| Předmět: |
Norcantharidin
Dose-Response Relationship Drug Molecular Structure Chemistry Stereochemistry Molecular Conformation Mtt method Maleic anhydride Antineoplastic Agents Bridged Bicyclo Compounds Heterocyclic Combinatorial chemistry Acylation Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Furan Drug Discovery Cancer cell Proton NMR Humans Structure–activity relationship Drug Screening Assays Antitumor Cell Proliferation |
| Zdroj: | Medicinal Chemistry. 10:376-381 |
| ISSN: | 1573-4064 |
| Popis: | Diels-Alder reaction between furan and maleic anhydride resulted in 5,6-dehydro norcantharidin, then norcantharidin was obtained by reduction. The substituted-carboxylic acid was condensed with N-aminothiourea in presence of phosphorus oxychloride, yielding 2-amino-1,3,4-thiadiazole derivatives. Novel norcantharidin derivatives were synthesized with acylation, then intramolecular condensation using norcantharidin (or 5,6-dehydro norcantharidin) and 2-amino- 1,3,4-thiadiazole derivatives. All the target compounds were confirmed by IR, (1)HNMR, ESI-MS and were reported for the first time. Norcantharidin derivatives antiproliferative assay was tested by MTT method against A549 and PC-3 cell lines. The results showed that all the norcantharidin derivatives displayed moderate inhibitory activities. |
| Databáze: | OpenAIRE |
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