Synthesis and Cytotoxicity of 2-Methyl-1-substituted-imidazo[4,5- g ]quinoline-4,9-dione and 7,8-dihydro-10 H -[1,4]oxazino[3′,4′:2,3]imidazo[4,5- g ]quinoline-5,12-dione Derivatives
| Autor: | Soyoung Park, Myung-Eun Suh, Min-Jung Kang, Hee-Won Yoo, Chong-Ock Lee |
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| Rok vydání: | 2000 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Tumor Cells Cultured medicine Humans Doxorubicin Cytotoxicity Molecular Biology Cisplatin Molecular Structure Organic Chemistry Quinoline Imidazoles Intercalating Agents In vitro Quinone chemistry Cell culture Quinolines Molecular Medicine Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 8:2079-2083 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(00)00132-2 |
| Popis: | 2-Methyl-1-substituted-imidazo[4,5- g ]quinoline-4,9-diones and 7,8-dihydro-10 H -[1,4]oxazino -[3′,4′:2,3]imidazo[4,5- g ]quinoline-5,12-dione ( 19 ) derivatives have been synthesized from 6,7-dichloro-5,8-quinolinedione for developing the new anticancer drugs. Our study on the cytotoxicity of imidazoquinolinedione derivatives has revealed that 7,8-dihydro-10 H -[1,4]oxazino-[3′,4′:2,3]imidazo[4,5- g ]quinoline-5,12-dione ( 19 ), a tetracyclic heteroquinone analogue, exhibited high cytotoxicity on human colon tumor cell (HCT 15) in vitro SRB assay. The IC 50 value of this compound was 0.026 μg/mL whereas those of doxorubicin and cisplatin were 0.023 μg/mL and 1.482 μg/mL, respectively. Meanwhile compounds 5 – 7 and 12 in the series of 1-substituted-imidazoquinolinediones showed relatively good activity on human brain tumor cell lines (XF 498). |
| Databáze: | OpenAIRE |
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