Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors.
Bioorg Med Chem Lett
; 28(8): 1320-1323, 2018 05 01.
Article
em En
| MEDLINE
| ID: mdl-29545100
ABSTRACT
In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and 3h possessed Topoisomerase II inhibition potency at 20⯵M. Mechanism study revealed that these compounds may function as Topo II catalytic inhibitors. It was found that the electron-withdrawing groups on the phenyl ring of compounds played an important role on enhancing both enzyme inhibition and cytotoxicity.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Rodanina
/
Carbazóis
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DNA Topoisomerases Tipo II
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Inibidores da Topoisomerase II
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article