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用作乏氧细胞辐射增敏剂的新型硝基吡嗪的合成与活性

Synthesis and activity of novel nitropyrazines for use as hypoxic cell radiosensitizers.

作者信息

Hartman G D, Hartman R D, Schwering J E, Saari W S, Engelhardt E L, Jones N R, Wardman P, Watts M E, Woodcock M

出版信息

J Med Chem. 1984 Dec;27(12):1634-9. doi: 10.1021/jm00378a018.

DOI:10.1021/jm00378a018
PMID:6389865
Abstract

A series of eight novel nitropyrazines has been prepared by oxidation of sulfoximine intermediates. The partition coefficient, one-electron reduction potential, sensitizer enhancement ratio, and chronic and acute aerobic cytotoxicity have been measured for each. Two representatives of this series were tested in the Ames test and were not found to be mutagenic.

摘要

通过氧化磺胺肟中间体制备了一系列八种新型硝基吡嗪。已对每种硝基吡嗪的分配系数、单电子还原电位、敏化剂增强率以及慢性和急性需氧细胞毒性进行了测定。对该系列中的两种代表性化合物进行了艾姆斯试验,未发现具有致突变性。

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