Document Type
Article
Abstract
A new adenine-substituted bromotyrosine-derived metabolite designated as aphrocallistin (1) has been isolated from the deep-water Hexactinellida sponge Aphrocallistes beatrix. Its structure was elucidated on the basis of spectral data and confirmed through a convergent, modular total synthetic route that is amenable toward future analogue preparation. Aphrocallistin inhibits the growth of a panel of human tumor cell lines with IC50 values ranging from 7.5 to >100 μM and has been shown to induce G1 cell cycle arrest in the PANC-1 pancreatic carcinoma cell line. Aphrocallistin has been fully characterized in the NCI cancer cell line panel and has undergone in Vitro ADME pharmacological profiling.
DOI
10.1021/np900183v (doi)
Publication Date
2009
Recommended Citation
To access the final edited and published work see http://dx.doi.org/10.1021/np900183v. This article may be cited as: Wright, A. E., Roth, G. P., Hoffman, J. K., Divlianska, D. B., Pechter, D., Sennett, S. H., Guzman, E. A., Linley, P., McCarthy, P. J., Pitts, T. P., Pomponi, S. A., & Reed, J K. (2009). Isolation, synthesis, and biological activity of Aphrocallistin, an adenine-substituted bromotyramine metabolite from the hexactinellida sponge Aphrocallistes beatrix. Journal of Natural Products, 72(6), 1178-1183. doi:10.1021/np900183v
Comments
Florida Atlantic University. Harbor Branch Oceanographic Institute contribution #1733.