Ring-closing metathesis for the synthesis of a highly G-quadruplex selective macrocyclic hexaoxazole having enhanced cytotoxic potency

Mavurapu Satyanarayana, Suzanne G. Rzuczek, Edmond J. LaVoie, Daniel S. Pilch, Angela Liu, Leroy-Fong Liu, Joseph E. Rice

研究成果: 雜誌貢獻文章

29 引文 斯高帕斯(Scopus)

摘要

The synthesis of a 24-membered macrocyclic hexaoxazole via ring-closing metathesis is described. The target compound selectively stabilizes G-quadruplex DNA with no detectable stabilization of duplex DNA. An MTT cytotoxicity assay indicated that this unsaturated macrocyclic hexaoxazole exhibits significant cytotoxicity toward P388, RPMI 8402, and KB3-1 cell lines with IC50 values of 45, 25, and 38 nM, respectively.

原文英語
頁(從 - 到)3802-3804
頁數3
期刊Bioorganic and Medicinal Chemistry Letters
18
發行號13
DOIs
出版狀態已發佈 - 七月 1 2008
對外發佈Yes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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