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硝基吡咯放射增敏剂:结构与功能的关系

Nitropyrrole radiosensitizers: structure function relationships.

作者信息

Raleigh J A, Chapman J D, Reuvers A P, Biaglow J E, Durand R E, Rauth A M

出版信息

Br J Cancer Suppl. 1978 Jun;3:6-10.

Abstract

Nitropyrrole derivatives have been tested as hypoxic cell radiosensitizers in vitro and in vivo. Radiosensitizing potential generally increases with nitropyrrole electron affinity. N-hydroxyethyl substitution decreases toxicity relative to N--CH3, N--CH2 CH3 and N--CH2 CH2 CH3 substitution. The most effective nitropyrrole tested in vivo is N-hydroxyethyl-2-cyano-5-nitropyrrole (NP-1).

摘要

硝基吡咯衍生物已在体外和体内作为乏氧细胞放射增敏剂进行了测试。放射增敏潜力通常随硝基吡咯电子亲和力的增加而增强。相对于N-CH3、N-CH2 CH3和N-CH2 CH2 CH3取代,N-羟乙基取代降低了毒性。体内测试的最有效的硝基吡咯是N-羟乙基-2-氰基-5-硝基吡咯(NP-1)。

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