Tetramethylpiperidine-substitution increases the antitumor activity of the riminophenazines for an acquired multidrug-resistant cell line

Authors: van Rensburg C.; Jooné G.; O'Sullivan J.

Source: Anti-Cancer Drug Design, Volume 15, Number 4, 2000 , pp. 303-306(4)

Publisher: Cognizant Communication Corporation

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Abstract:

The multidrug resistance (MDR)-neutralizing and cytotoxic properties of five tetramethylpiperidine (TMP-substituted phenazines were compared with those of their corresponding isopropyl-substituted analogues using a P-glycoprotein (P-gp)-expressing small cell lung cancer cell line (H69/LX4). All of the TMP-substituted phenazines tested outperformed their isopropyl analogues with respect to both cytotoxic and chemosensitizing properties, indicating the importance of TMP-substitution when designing novel riminophenazines with increased activity against MDR cancer cell lines. Of the TMP-substituted phenazines tested, B4112, chlorinated at position 3 of the phenyl- and anilino-rings, had the most potent anti-cancer activity in vitro, making this agent a potential candidate for evaluation in experimental and clinical oncology.

Document Type: Research article

Affiliations: 1: Department of Chemistry, University College, Belfield, Dublin, Ireland

Publication date: 2000-08-01