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Chemical synthesis and cytotoxicity of dihydroxylated cyclopentenone analogues of neocarzinostatin chromophore.

Abstract
Compounds containing the naphthoate moiety of Neocarzinostatin chromophore or 2-hydroxynaphthoate have been synthesized and evaluated for cytotoxic activity against a leukemia cell line and a small panel of human-tumor cell lines. Those compounds containing a cyclopentenone moiety were active, with the carbonyl group being essential for biological activity.
AuthorsMichael D Urbaniak, Lisa M Frost, John P Bingham, Lloyd R Kelland, John A Hartley, Derek N Woolfson, Stephen Caddick
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 13 Issue 12 Pg. 2025-7 (Jun 16 2003) ISSN: 0960-894X [Print] England
PMID12781188 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antibiotics, Antineoplastic
  • Cyclopentanes
  • Enediynes
  • neocarzinostatin chromophore
  • Zinostatin
  • cyclopentenone
Topics
  • Antibiotics, Antineoplastic (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Cyclopentanes (chemistry, pharmacology)
  • Drug Screening Assays, Antitumor
  • Enediynes
  • HT29 Cells
  • Humans
  • Hydroxylation
  • Inhibitory Concentration 50
  • K562 Cells
  • Zinostatin (analogs & derivatives, chemical synthesis, chemistry, pharmacology)

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