Fungal phenalenones inhibit HIV-1 integrase
| Autor: | Miki Isozaki, Hua Yan, Haruo Tanaka, Rokuro Masuma, Kazuro Shiomi, Tomoko Chiba, Yuichi Yamaguchi, Yoshihiro Kitamura, Hiroshi Tomoda, Ryosuke Matsui, Wataru Sugiura, Takahiro Sugai, Satoshi Omura, Harumi Chiba |
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| Rok vydání: | 2005 |
| Předmět: |
Antifungal Agents
Stereochemistry Integrase inhibitor HIV Integrase Naphthalenes chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Polycyclic Compounds Enzyme Inhibitors Cytotoxicity IC50 Pharmacology biology Chemistry Acetal virus diseases Ketones Phenalenes biology.organism_classification In vitro Integrase Biochemistry Enzyme inhibitor Penicillium biology.protein |
| Zdroj: | The Journal of antibiotics. 58(1) |
| ISSN: | 0021-8820 |
| Popis: | A phenalenone compound, atrovenetinone methyl acetal, was isolated from a culture broth of Penicillium sp. FKI-1463 as an HIV-1 integrase inhibitor, and it showed anti-HIV activity in vitro. HIV-1 integrase inhibition and anti-HIV activity of two other natural phenalenones were also studied. Among the tested compounds, funalenone inhibited HIV-1 integrase with an IC50 value of 10 microM and showed the best selectivity (anti-HIV, IC50=1.7 microM; cytotoxicity, IC50=87 microM). |
| Databáze: | OpenAIRE |
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