Synthesis and antiproliferative action of a novel series of maprotiline analogues. Academic Article uri icon

Overview

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.

publication date

  • November 9, 2013

Research

keywords

  • Adrenergic Uptake Inhibitors
  • Antineoplastic Agents
  • Burkitt Lymphoma
  • Cell Proliferation
  • Maprotiline

Identity

Scopus Document Identifier

  • 84889561054

Digital Object Identifier (DOI)

  • 10.1016/j.ejmech.2013.10.076

PubMed ID

  • 24333581

Additional Document Info

volume

  • 71