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- W2012576543 abstract "The trans-fused gamma-lactone ring of etoposide is readily epimerized to its cis epimer, which is biologically inactive, or is metabolized to the inactive ring-opened hydroxy acids. Modification of this gamma-lactone ring of 4 beta-(arylamino)-4'-O-demethyl-4-desoxypodophyllotoxin resulted in several compounds (15-16, 21-22, and 24) that should block this epimerization and the resulting biological deactivation. In a topoisomerase II inhibition assay, compounds 21, 22, and 24 showed comparable activity to etoposide. In a protein-linked DNA complex formation assay, compounds 21 and 22 were more active than etoposide." @default.
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- W2012576543 date "1994-01-01" @default.
- W2012576543 modified "2023-09-24" @default.
- W2012576543 title "Antitumor agents. 144. New .gamma.-lactone ring-modified arylamino etoposide analogs as inhibitors of human DNA topoisomerase II" @default.
- W2012576543 doi "https://doi.org/10.1021/jm00028a012" @default.
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