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Identification of a new natural camptothecin analogue in targeted screening for HIF-1 alpha inhibitors

  1. Author:
    Klausmeyer, P.
    McCloud, T. G.
    Melillo, G.
    Scudiero, D. A.
    Cardellina, J. H.
    Shoemaker, R. H.

  2. Author Address

    NCI, SAIC Frederick, Nat Prod Support Grp, Frederick, MD 21702 USA. NCI, SAIC Frederick, DTP Tumor Hypoxia Lab, Frederick, MD 21702 USA. NCI, SAIC Frederick, In Vitro Cell Line Screening Program, Frederick, MD 21702 USA. NCI, Screnning Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diagnosis,FCRDC, Frederick, MD 21701 USA.;McCloud, TG, NCI, SAIC Frederick, Nat Prod Support Grp, Frederick, MD 21702 USA.;mccloud@dtpax2.ncifcrf.gov
    1. Year: 2007
    2. Date: Jan
  2. Journal: Planta Medica
    1. 73
    2. 1
    3. Pages: 49-52
  4. Type of Article: Article
  5. ISSN: 0032-0943
  1. Abstract:

    Screening to detect compounds that inhibit the HIF-1 a transcriptional activation pathway identified an extract of Ophiorrhiza trichocarpon for investigation. A high throughput dereplication strategy was employed, involving chromatography with spectral data acquisition supported by bioactivity testing and literature referencing, which led to rapid identification of camptothecin (1) and three analogues (2-4) as the active compounds. 9,10-Methylenedioxy-(20S)-camptothecin (4) was found for the first time from a plant.

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External Sources

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  2. DOI: 10.1055/s-2006-951767
  3. View record in Web of Science®
  4. WOS: 000244086400008

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