Synthesis and biological evaluation of phenyl substituted polyoxygenated xanthone derivatives as anti-hepatoma agents
| Autor: | Jian Kang, Run-Hui Liu, Hu Yuan, Zhi-Jun Zhu, Bing-Yang Chen, Qingyan Sun, Rongcai Yue, Xing Yuan, Ming Dai, Wei-Dong Zhang |
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| Rok vydání: | 2013 |
| Předmět: |
Carcinoma
Hepatocellular Stereochemistry Xanthones Antineoplastic Agents Apoptosis Xanthone Derivatives Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Drug Discovery Xanthone Tumor Cells Cultured medicine Humans Structure–activity relationship Cytotoxicity Cell Proliferation 030304 developmental biology Pharmacology 0303 health sciences Dose-Response Relationship Drug Molecular Structure Chemistry Liver Neoplasms Organic Chemistry Hep G2 Cells General Medicine medicine.disease 3. Good health Biochemistry 030220 oncology & carcinogenesis Hepatocellular carcinoma Hepatic stellate cell Drug Screening Assays Antitumor Selectivity |
| Zdroj: | European Journal of Medicinal Chemistry. 69:159-166 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2013.08.020 |
| Popis: | A series of novel derivatives of phenyl substituted tetramethoxy xanthone were synthesized and evaluated for their in vitro cytotoxicity against human hepatocellular carcinoma (HCC) and non-tumor hepatic cells. Among these derivatives, compound 6 was more potent than positive control 5-fluorouracil (5-Fu) on QGY-7703 and SMMC-7721 cells with IC50 values of 6.27 μM, 7.50 μM and 15.56 μM, 14.55 μM, respectively. Furthermore, compounds 6, 14, 16, and 29 exhibited much better selectivity toward the normal hepatic cell line QSG-7701 than 5-Fu. Additionally, compound 6 significantly induced cell apoptosis in QGY-7703 cells. Our findings suggested that these phenylxanthone derivatives may hold promise as chemotherapeutic agents for the treatment of human HCC. |
| Databáze: | OpenAIRE |
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