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

青蒿素衍生的二聚磷酸酯作为有效的抗巨细胞病毒 (抗 CMV) 和抗癌剂:结构活性研究

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

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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