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Artemisinin-derived dimer phosphate esters as potent anti-cytomegalovirus (anti-CMV) and anti-cancer agents: a structure-activity study. Bioorg Med Chem 2013 Jul 01;21(13):3702-7

Date

05/16/2013

Pubmed ID

23673218

Pubmed Central ID

PMC3685872

DOI

10.1016/j.bmc.2013.04.027

Scopus ID

2-s2.0-84878563527 (requires institutional sign-in at Scopus site)   36 Citations

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.

Author List

Mott BT, He R, Chen X, Fox JM, Civin CI, Arav-Boger R, Posner GH

Author

Ravit Boger MD Chief, Professor in the Pediatrics department at Medical College of Wisconsin




MESH terms used to index this publication - Major topics in bold

Antineoplastic Agents
Antiviral Agents
Artemisinins
Cytomegalovirus
Cytomegalovirus Infections
Dimerization
Esters
Humans
Jurkat Cells
Leukemia
Phosphates