A Dual Topoisomerase Inhibitor of Intense Pro-Apoptotic and Antileukemic Nature for Cancer Treatment.
ChemMedChem
; 12(5): 347-352, 2017 03 07.
Article
em En
| MEDLINE
| ID: mdl-28099785
ABSTRACT
Classic cytotoxic drugs remain indispensable instruments in antitumor therapy due to their effectiveness and a more prevalent insensitivity toward tumor resistance mechanisms. Herein we describe the favorable properties of 6-(N,N-dimethyl-2-aminoethoxy)-11-(3,4,5-trimethoxyphenyl)pyrido[3,4-c][1,9]phenanthroline (P8-D6), a powerful inducer of apoptosis caused by an equipotent inhibition of human topoisomerase I and II activities. A broad-spectrum effect against human tumor cell lines at nanomolar concentrations, as well as strong antileukemic effects, were shown to be superior to those of marketed topoisomerase-targeting drugs and dual topoisomerase inhibitors in clinical trials. The facile four-step synthesis, advantageous drugability properties, and initial inâ
vivo data encourage the application of P8-D6 in appropriate animal tumor models and further drug development.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores da Topoisomerase I
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Inibidores da Topoisomerase II
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Naftalenos
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Antineoplásicos
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article