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.
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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)
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Copyright | Copyright © 2013 Elsevier Ltd. All rights reserved. |
Chemical References |
- Antineoplastic Agents
- Antiviral Agents
- Artemisinins
- Esters
- Phosphates
- artemisinin
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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)
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