2. Academic Validation
  3. Antineoplastic agents. 380. Isolation and X-ray crystal structure determination of isoaaptamine from the Republic of Singapore Hymeniacidon sp. and conversion to the phosphate prodrug hystatin 1

Antineoplastic agents. 380. Isolation and X-ray crystal structure determination of isoaaptamine from the Republic of Singapore Hymeniacidon sp. and conversion to the phosphate prodrug hystatin 1

  • J Nat Prod. 2004 Mar;67(3):506-9. doi: 10.1021/np0204592.
George R Pettit 1,  Holger Hoffmann,  James McNulty,  Kerianne C Higgs,  Alison Murphy,  David J Molloy,  Delbert L Herald,  Michael D Williams,  Robin K Pettit,  Dennis L Doubek,  John N A Hooper,  Leslie Albright,  Jean M Schmidt,  Jean-Charles Chapuis,  Larry P Tackett
Affiliations

Affiliation

  • 1 Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona 85287-2404, USA.
PMID: 15043446 DOI: 10.1021/np0204592
Abstract

By use of bioassay (murine P388 lymphocytic leukemia cell line) guided isolation procedures, extracts of the Republic of Singapore marine Sponge Hymeniacidon sp. were found to contain demethyloxyaaptamine (1) and aaptamine (3) as prominent Cancer cell growth inhibitory constituents accompanied by the trace, albeit more active, component isoaaptamine (4). The isolation, X-ray structure elucidation, and antineoplastic and antimicrobial activities of isoaaptamine (4) have been summarized. Because of instability, isoaaptamine (4) was converted to a stable sodium phosphate prodrug designated hystatin 1 (7).

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