Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors
| Autor: | Zu-Ping Wu, De-Qing Shen, Lin-Kun An, Zhi-Shu Huang, Xi-Wei Wu, Xiang-Zhang Bu, Zeng-Yun An, Lian-Quan Gu |
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| Rok vydání: | 2010 |
| Předmět: |
Nitrogen
Cell Chemical synthesis Inhibitory Concentration 50 Cell Line Tumor Drug Discovery medicine Humans Cell Proliferation Pharmacology chemistry.chemical_classification biology Topoisomerase Organic Chemistry Indolizines Biological activity General Medicine In vitro medicine.anatomical_structure Enzyme DNA Topoisomerases Type I chemistry Biochemistry Cell culture Drug Design biology.protein Phthalazines Topoisomerase I Inhibitors Breast carcinoma |
| Zdroj: | European Journal of Medicinal Chemistry. 45:3938-3942 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2010.05.048 |
| Popis: | A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds. |
| Databáze: | OpenAIRE |
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