The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins.

Ashoorzadeh A; Atwell GJ; Pruijn FBWilson WRTercel MDenny WAStevenson RJ

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The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins.

机译：The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins.

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A series of 3-substituted (5-nitro-2,3-dihydro-1H-benzo[e]indol-1-yl)methyl sulfonate (nitroCBI) prodrugs containing sulfonate leaving groups undergo hypoxia-selective metabolism to form potent DNA minor groove alkylating agents. They were evaluated (along with chloride leaving group analogs for comparison) for their cytotoxicity against cultures of SKOV3 and HT29 human tumor cell lines under both aerobic and hypoxic conditions. Sulfonates with neutral side chains (e.g., 5,6,7-trimethoxyindole; TMI) show consistently higher hypoxic cytotoxicity ratios (HCRs) (34-246) than the corresponding chloro analogs (2.8-3.1) in SKOV3 cells, but these trends do not hold for compounds with cationic or polar neutral side chains.

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《Bioorganic and medicinal chemistry》 |2011年第16期|4851-4860|共10页
作者
Ashoorzadeh A; Atwell GJ; Pruijn FBWilson WRTercel MDenny WAStevenson RJ;
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Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.;

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正文语种英语
中图分类药学;
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The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins.

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