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

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.

• Authors: Bryan T Mott, Ran He, Xiaochun Chen, Jennifer M Fox, Curt I Civin, Ravit Arav-Boger, Gary H Posner
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 21 Issue 13 Pg. 3702-7 (Jul 01 2013) ISSN: 1464-3391 [Electronic] England
• PMID: 23673218 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Antiviral Agents
• Artemisinins
• Esters
• Phosphates
• artemisinin

Topics

• Antineoplastic Agents (chemistry, pharmacology)
• Antiviral Agents (chemistry, pharmacology)
• Artemisinins (chemistry, pharmacology)
• Cytomegalovirus (drug effects)
• Cytomegalovirus Infections (drug therapy)
• Dimerization
• Esters
• Humans
• Jurkat Cells
• Leukemia (drug therapy)
• Phosphates (chemistry, pharmacology)