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Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum

Publication ,  Journal Article
Singh, SB; Zink, DL; Guan, Z; Collado, J; Pelaez, F; Felock, PJ; Hazuda, DJ
Published in: Helvetica Chimica Acta
November 20, 2003

HIV-1 Integrase is a critical enzyme for replication of HIV, and its inhibition is one of the most promising new drug targets for anti-retroviral therapy with potentially significant advantages over existing therapies. Xanthoviridicatins E (1) and F (2) are two novel polyketide natural products that were isolated from a fermentation broth of an endophytic strain of Penicillium chrysogenum isolated from the living leaves collected in Peru. These compounds are new members of the unsymmetrical xanthoviridicatin family represented by the broader xanthomegnin family. Xanthoviridicatins E and F inhibited the cleavage reaction of HIV-1 integrase with an IC50 of 6 and 5 μM, respectively. The bioassay-directed isolation, structure elucidation, and HIV-1 inhibitory activity of these compounds are described.

Duke Scholars

Published In

Helvetica Chimica Acta

DOI

ISSN

0018-019X

Publication Date

November 20, 2003

Volume

86

Issue

10

Start / End Page

3380 / 3385

Related Subject Headings

  • General Chemistry
  • 34 Chemical sciences
  • 03 Chemical Sciences
 

Citation

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Singh, S. B., Zink, D. L., Guan, Z., Collado, J., Pelaez, F., Felock, P. J., & Hazuda, D. J. (2003). Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum. Helvetica Chimica Acta, 86(10), 3380–3385. https://doi.org/10.1002/hlca.200390281
Singh, S. B., D. L. Zink, Z. Guan, J. Collado, F. Pelaez, P. J. Felock, and D. J. Hazuda. “Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum.” Helvetica Chimica Acta 86, no. 10 (November 20, 2003): 3380–85. https://doi.org/10.1002/hlca.200390281.
Singh SB, Zink DL, Guan Z, Collado J, Pelaez F, Felock PJ, et al. Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum. Helvetica Chimica Acta. 2003 Nov 20;86(10):3380–5.
Singh, S. B., et al. “Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum.” Helvetica Chimica Acta, vol. 86, no. 10, Nov. 2003, pp. 3380–85. Scopus, doi:10.1002/hlca.200390281.
Singh SB, Zink DL, Guan Z, Collado J, Pelaez F, Felock PJ, Hazuda DJ. Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum. Helvetica Chimica Acta. 2003 Nov 20;86(10):3380–3385.
Journal cover image

Published In

Helvetica Chimica Acta

DOI

ISSN

0018-019X

Publication Date

November 20, 2003

Volume

86

Issue

10

Start / End Page

3380 / 3385

Related Subject Headings

  • General Chemistry
  • 34 Chemical sciences
  • 03 Chemical Sciences