Design of pH responsive clickable prodrugs applied to histone deacetylase inhibitors: a new strategy for anticancer therapy.
Eur J Pharm Biopharm
; 85(3 Pt B): 862-72, 2013 Nov.
Article
em En
| MEDLINE
| ID: mdl-23537575
ABSTRACT
The aim of this study was to develop clickable prodrugs bearing a tunable pH responsive linker designed for acidic pH-mediated release of histone deacetylase inhibitors. HDACi are an important class of molecules belonging to the epigenetic modulators used for innovative cancer strategies. The behavior of these prodrugs was determined by a bioluminescence resonance energy transfer assay in living tumor cells. This work demonstrated that this innovative type of clickable prodrugs entered cancer cells and showed restored anti proliferative properties attributed to the effective release of the HDAC inhibitors. A correlation between kinetic studies, dose responses, and biological activities was obtained, making such clickable prodrugs good candidates for new strategies in epigenetic-oriented anticancer therapies.
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Base de dados:
MEDLINE
Assunto principal:
Pró-Fármacos
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Desenho de Fármacos
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Inibidores de Histona Desacetilases
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Química Click
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Neoplasias Pulmonares
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Neoplasias
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Antineoplásicos
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article