Synthesis and antiproliferative action of a novel series of maprotiline analogues.
Eur J Med Chem
; 71: 333-53, 2014 Jan.
Article
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| MEDLINE
| ID: mdl-24333581
ABSTRACT
The synthesis of a diverse library of compounds structurally related to maprotiline, a norepinephrine reuptake transporter (NET) selective antidepressant which has recently been identified as a novel in vitro antiproliferative agent against Burkitt's lymphoma (BL) cell lines is reported. A series of 9,10-dihydro-9,10-ethanoanthracenes were synthesised with modifications to the bridge of the dihydroethanoanthracene structure and with alterations to the basic side chain. A number of compounds were found to reduce cell viability to a greater extent than maprotiline in BL cell lines. In addition a related series of novel 9-substituted anthracene compounds were investigated as intermediates in the synthesis of 9,10-dihydro-9,10-ethanoanthracenes. These compounds proved the most active from the screen and were found to exert a potent caspase-dependant apoptotic effect in the BL cell lines, while having minimal effect on the viability of peripheral blood mononuclear cells (PBMCs). Compounds also displayed activity in multi-drug resistant (MDR) cells.
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Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Linfoma de Burkitt
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Inhibidores de Captación Adrenérgica
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Proliferación Celular
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Maprotilina
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Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2014
Tipo del documento:
Article
País de afiliación:
Irlanda