کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582675 | 981085 | 2011 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins](/preview/png/10582675.png)
چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4851-4860
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4851-4860
نویسندگان
Amir Ashoorzadeh, Graham J. Atwell, Frederik B. Pruijn, William R. Wilson, Moana Tercel, William A. Denny, Ralph J. Stevenson,