| Autor: |
Monsen PJ; Department of Chemistry , University of Louisville , 2320 South Brook Street , Louisville , Kentucky 40292 , United States., Luzzio FA; Department of Chemistry , University of Louisville , 2320 South Brook Street , Louisville , Kentucky 40292 , United States. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of natural products [J Nat Prod] 2018 Aug 24; Vol. 81 (8), pp. 1905-1909. Date of Electronic Publication: 2018 Jul 20. |
| DOI: |
10.1021/acs.jnatprod.8b00284 |
| Abstrakt: |
Annonacin (1) was isolated from the North American pawpaw ( Asimina triloba), as reported earlier from these laboratories. Natural 1 was submitted to the rat aortic ring bioassay for evaluation of antiangiogenic activity and was found to inhibit microvessel growth (IC 50 value of 3 μM). 4,10,15,20-Tetraazido derivatives of 1 were prepared by permesylation followed by azide displacement or by iodination followed by azide displacement. The tetraazide derived from mesylation/azidation was antiangiogenic, while that derived from iodination/azidation exhibited no appreciable activity. The membrane permeability of natural 1 was evaluated using the parallel artificial membrane permeability assay and was found to be marginally permeable as compared to several clinically relevant compounds. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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