Antitumor agents, 107. New cytotoxic 4-alkylamino analogues of 4'-demethyl-epipodophyllotoxin as inhibitors of human DNA topoisomerase II.
J Nat Prod
; 52(3): 606-13, 1989.
Article
em En
| MEDLINE
| ID: mdl-2550587
ABSTRACT
A series of analogues of etoposide, the C-4 amino- and alkylamino-substituted 4'-demethyl-epipodophyllotoxins, have been synthesized and studied for their activity to inhibit type II human DNA topoisomerase as well as their activity in causing cellular protein-linked DNA breakage. Substitution of the glycosidic moiety of 1 by a 2"-hydroxyethylamino or 2"-methoxyethylamino chain at the C-4 beta position resulted in potent inhibitors of the human DNA topoisomerase II. This inhibitory activity correlates reasonably well with their activity in causing protein-linked DNA breakage in KB cells. The in vitro cytotoxicity (KB) appears to have no correlation with the inhibitory activity of the human DNA topoisomerase II.
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Base de dados:
MEDLINE
Assunto principal:
Podofilotoxina
/
Inibidores da Topoisomerase II
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
1989
Tipo de documento:
Article