Hypoxia-selective antitumor agents. 10. Bis (nitroimidazoles) and related bis (nitroheterocycles): development of derivatives with higher rates of metabolic activation …

MP Hay, HH Lee, WR Wilson, PB Roberts…

文献索引：Hay, Michael P.; Lee, Ho H.; Wilson, William R.; Roberts, Peter B.; Denny, William A. Journal of Medicinal Chemistry, 1995 , vol. 38, # 11 p. 1928 - 1941

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被引用次数: 27

摘要

1H-yl) ethyll-4-(2-nitroimidazol-1H-yl) butanamide (4), a novel hypoxic cell cytotoxin and radiosensitizer, have been prepared and evaluated for hypoxia-selective cytotoxicity and hypoxic cell radiosensitization in vitro. The new derivatives were designed to overcome the low aqueous solubility of 4 and its slow kinetics of killing under hypoxia. The nitroheterocycle unit had a significant effect on solubility, with 3-nitrotriazoles being about ...