Novel trifluoromethylated 9-amino-3,4-dihydroacridin-1(2H)-ones act as covalent poisons of human topoisomerase IIα.

doi:10.1016/j.bmcl.2016.12.011

Paper

DOI: 10.1016/j.bmcl.2016.12.011

Novel trifluoromethylated 9-amino-3,4-dihydroacridin-1(2H)-ones act as covalent poisons of human topoisomerase IIα.

Published Feb 1, 2017 · Lorena Infante Lara, A. Sledge, A. Laradji

Bioorganic & medicinal chemistry letters

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Abstract

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In Vitro Study

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Novel trifluoromethylated 9-amino-3,4-dihydroacridin-1(2H)-one derivatives act as covalent topoisomerase II poisons, enhancing DNA cleavage 5.5-8.5-fold over baseline, but are less potent than ams

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Assembly of Biaryl Amines via Mild Copper-Catalyzed Coupling of Anilines with (Hetero)aryl Chlorides/Bromides.

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