Total synthesis and evaluation of lamellarin α 20-Sulfate analogues
| Autor: | M. Venkata Rami Reddy, Frederic D. Bushman, Christian P. Ridley, D. John Faulkner, Genalyn Rocha |
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| Rok vydání: | 2002 |
| Předmět: |
Topoisomerase Inhibitors
Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Heterocyclic Compounds 4 or More Rings Biochemistry Structure-Activity Relationship Coumarins Drug Discovery Tumor Cells Cultured Humans HIV Integrase Inhibitors Cytotoxicity Molecular Biology chemistry.chemical_classification Molluscum contagiosum virus biology Chemistry Alkaloid Organic Chemistry Total synthesis Biological activity Isoquinolines Integrase Enzyme Enzyme inhibitor biology.protein Molecular Medicine Drug Screening Assays Antitumor Lactone HeLa Cells |
| Zdroj: | Bioorganic & Medicinal Chemistry. 10:3285-3290 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(02)00237-7 |
| Popis: | In order to explore the influence of sulfate groups on the bioactivity profiles of marine alkaloids of the lamellarin class, three such alkaloids, lamellarin alpha, lamellarin alpha 13,20-disulfate and lamellarin H, were synthesized and their activities against HIV-1 integrase and cancer cell lines were compared with those of lamellarin alpha 20-sulfate, which is a selective inhibitor of HIV-1 integrase. Lamellarin alpha does not inhibit HIV-1 integrase but shows moderate cytotoxicity with good cell line selectivity. Lamellarin alpha 13,20-disulfate is a moderate inhibitor of both HIV-1 integrase and cancer cell lines. Lamellarin H is a more potent inhibitor of HIV-1 integrase but lacked the specificity required to be medicinally useful. |
| Databáze: | OpenAIRE |
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