Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
Bioorg Med Chem Lett
; 27(11): 2308-2312, 2017 06 01.
Article
em En
| MEDLINE
| ID: mdl-28434764
ABSTRACT
Piperlongumine (PL) is a natural alkaloid with broad biological activities. Twelve analogues have been designed and synthesized with non-substituted benzyl rings or heterocycles in this work. Most of the compounds showed better anticancer activities than the parent PL without apparent toxicity in normal cells. Elevation of cellular ROS levels was one of the main anticancer mechanisms of these compounds. Cell apoptosis and cell cycle arrest for the best compound ZM90 were evaluated and similar mechanism of action with PL was demonstrated. The SAR was also characterized, providing worthy directions for further optimization of PL compounds.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Dioxolanos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
China