Activity profile of the novel aziridinylbenzoquinones MeDZQ and RH1 in human tumour xenografts.
Cummings, Jeffrey Ritchie, Alison Butler, John Ward, Timothy H Langdon, Simon
Cummings, Jeffrey
Ritchie, Alison
Butler, John
Ward, Timothy H
Langdon, Simon
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Abstract
BACKGROUND: RH1 and MeDZQ represent novel aziridinylbenzoquinones that can be activated by DT-diaphorase to form unique DNA lesions. RH1 is due to enter a phase 1 clinical trial in the United Kingdom in the summer of 2003, where pharmacodynamic monitoring of DT-diaphorase will be performed. MATERIALS AND METHODS: The antitumour efficacy of RH1 and MeDZQ has been studied in 4 human xenografts (3 non-small cell lung cancer and 1 colon cancer), and compared to the level of constitutive DT-Diaphorase activity measured by the DCPIP assay. RESULTS: The 4 xenografts exhibited a wide range of DT-diaphorase activity (4.8-303 nmol/min/mg). Greater antitumour activity was recorded in the xenografts expressing high levels of DT-diaphorase (e.g. NX002, DT-diaphorase activity, 303 +/- 52 nmol/min/mg, T/C to MeDZQ, 33.3% and to RH1, 43.4%). CONCLUSION: These data add in vivo support to a role for DT-Diaphorase in the antitumour activity of RH1.
Description
Date
2009-09-23T11:45:22Z
Publisher
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Keywords
Lung Cancer
Xenograft Model Antitumour Assays
Colonic Cancer
Xenograft Model Antitumour Assays
Colonic Cancer
Type
Article
Citation
Activity profile of the novel aziridinylbenzoquinones MeDZQ and RH1 in human tumour xenografts., 23 (5A):3979-83 Anticancer Res.