Unknown

Dataset Information

0

An artemisinin-derived dimer has highly potent anti-cytomegalovirus (CMV) and anti-cancer activities.


ABSTRACT: We recently reported that two artemisinin-derived dimers (dimer primary alcohol 606 and dimer sulfone 4-carbamate 832-4) are significantly more potent in inhibiting human cytomegalovirus (CMV) replication than artemisinin-derived monomers. In our continued evaluation of the activities of artemisinins in CMV inhibition, twelve artemisinin-derived dimers and five artemisinin-derived monomers were used. Dimers as a group were found to be potent inhibitors of CMV replication. Comparison of CMV inhibition and the slope parameter of dimers and monomers suggest that dimers are distinct in their anti-CMV activities. A deoxy dimer (574), lacking the endoperoxide bridge, did not have any effect on CMV replication, suggesting a role for the endoperoxide bridge in CMV inhibition. Differences in anti-CMV activity were observed among three structural analogs of dimer sulfone 4-carbamate 832-4 indicating that the exact placement and oxidation state of the sulfur atom may contribute to its anti-CMV activity. Of all tested dimers, artemisinin-derived diphenyl phosphate dimer 838 proved to be the most potent inhibitor of CMV replication, with a selectivity index of approximately 1500, compared to our previously reported dimer sulfone 4-carbamate 832-4 with a selectivity index of about 900. Diphenyl phosphate dimer 838 was highly active against a Ganciclovir-resistant CMV strain and was also the most active dimer in inhibition of cancer cell growth. Thus, diphenyl phosphate dimer 838 may represent a lead for development of a highly potent and safe anti-CMV compound.

SUBMITTER: He R 

PROVIDER: S-EPMC3164168 | biostudies-literature | 2011

REPOSITORIES: biostudies-literature

altmetric image

Publications

An artemisinin-derived dimer has highly potent anti-cytomegalovirus (CMV) and anti-cancer activities.

He Ran R   Mott Bryan T BT   Rosenthal Andrew S AS   Genna Douglas T DT   Posner Gary H GH   Arav-Boger Ravit R  

PloS one 20110831 8


We recently reported that two artemisinin-derived dimers (dimer primary alcohol 606 and dimer sulfone 4-carbamate 832-4) are significantly more potent in inhibiting human cytomegalovirus (CMV) replication than artemisinin-derived monomers. In our continued evaluation of the activities of artemisinins in CMV inhibition, twelve artemisinin-derived dimers and five artemisinin-derived monomers were used. Dimers as a group were found to be potent inhibitors of CMV replication. Comparison of CMV inhib  ...[more]

Similar Datasets

| S-EPMC2683803 | biostudies-literature
| S-EPMC3393438 | biostudies-literature
| S-EPMC7496903 | biostudies-literature
| S-EPMC4074917 | biostudies-literature
| S-EPMC4277730 | biostudies-literature
| S-EPMC6021623 | biostudies-literature
| S-EPMC5600906 | biostudies-literature
| S-EPMC4910920 | biostudies-literature
| S-EPMC3985958 | biostudies-literature
| S-EPMC3041771 | biostudies-literature