Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: A structure-activity study

Bryan T. Mott, Ran He, Xiaochun Chen, Jennifer M. Fox, Curt I. Civin, Ravit Arav-Boger, Gary H. Posner

Research output: Contribution to journalArticle

Abstract

We recently reported the anti-cancer and anti-cytomegalovirus (CMV) activity of artemisinin-derived trioxane diphenylphosphate dimer 838. To probe the relationship between chemical structure and anti-CMV and anti-cancer activities, we now report synthesis and evaluation of a series of eight new dimer phosphate ester analogs of 838. This series of novel molecules was screened against human foreskin fibroblasts (HFFs) infected with CMV and against the human Jurkat T cell acute lymphoblastic leukemia cell line. This SAR study confirms the very high anti-CMV and anti-cancer potencies of dimer diphenyl phosphate ester 838 without its being toxic to normal cells.

Original languageEnglish (US)
Pages (from-to)3702-3707
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number13
DOIs
StatePublished - Jul 1 2013

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Keywords

  • Artemisinin-derived dimmer
  • CMV
  • Leukemia
  • Phosphate ester

ASJC Scopus subject areas

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

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