Water-Soluble Camptothecin Derivatives that Are Intrinsic Topoisomerase I Poisons

Nicolas J. Rahier, Brian M. Eisenhauer, Rong Gao, Shannon H. Jones, Sidney M. Hecht

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

(Matrix presented) In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.

Original languageEnglish (US)
Pages (from-to)321-324
Number of pages4
JournalOrganic Letters
Volume6
Issue number3
DOIs
StatePublished - Feb 5 2004
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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