New candidaspongiolides, tedanolide analogues that selectively inhibit melanoma cell growth.

Abstract

Extracts of the sponge genus Candidaspongia showed selective cytotoxicity toward melanoma cells in the NCI 60-cell-line screen. Continued investigation of the Candidaspongia sp. extracts led to the isolation of three new tedanolide analogues, precandidaspongiolides A (1) and B (2) and candidaspongiolide B (4), as well as candidaspongiolide A (3) and tedanolide (5). Semisynthetic derivatives were also generated to develop SAR. Candidaspongiolides A/B were the most potent and showed low nanomolar activity against several melanoma cell lines.

• Authors: Emily L Whitson, Kristen M Pluchino, Matthew D Hall, James B McMahon, Tawnya C McKee
• Journal: Organic letters (Org Lett) Vol. 13 Issue 13 Pg. 3518-21 (Jul 01 2011) ISSN: 1523-7052 [Electronic] United States
• PMID: 21644548 (Publication Type: Journal Article, Research Support, N.I.H., Intramural)

Chemical References

• Macrolides
• candidaspongiolide
• tedanolide

Topics

• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Humans
• Macrolides (chemical synthesis, chemistry, pharmacology)
• Melanoma (pathology)
• Structure-Activity Relationship