Evaluation of various types of new hypoxic cell sensitizers using the EMT6 single cell-spheroid-solid tumour system.
Evaluation of various types of new hypoxic cell sensitizers using the EMT6 single cell-spheroid-solid tumour system.
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使用EMT6单细胞-球体-实体瘤系统评价各类新型缺氧细胞敏化剂。
DOI：
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发表时间：
1987
期刊：
影响因子：
--
通讯作者：
M. Abe
中科院分区：
文献类型：
--
作者：
Y. Shibamoto;S. Nishimoto;F. Mi;K. Sasai;T. Kagiya;M. Abe
在体外和体内与米索硝唑（misonidazole， MISO）、SR-2508、Ro 03-8799和ANT（2-氨基-5-硝基噻唑）比较，对日本1980 - 1985年间开发的11种新型缺氧细胞增敏剂进行了评价。新化合物包括2-硝基咪唑核苷类似物、硝基三唑和其他硝基芳烃、非硝基化合物和易于插入DNA的电子亲和化合物。EMT6单细胞的增敏活性不仅与还原电位有关，而且与某些化合物与非蛋白巯基的反应性有关。敏化剂还使用EMT6球体和实体肿瘤进行了测试。单细胞、球状体和实体肿瘤的增敏剂增强比（SERs）的变化模式可分为两种类型：(1)三种检测系统的SERs相似；(2) SERs降低的顺序为：单细胞、球状体、实体瘤。只有硝基咪唑和硝基三唑衍生物属于前一类。含有糖类似物成分的2-硝基咪唑类药物RK-28和RK-29在体内的作用与MISO基本相当。3-和4-硝基三唑衍生物也有明确的体内效应。
Eleven new hypoxic cell sensitizers representative of those developed in Japan between 1980 and 1985 were evaluated in vitro and in vivo in comparison with misonidazole (MISO), SR-2508, Ro 03-8799, and ANT (2-amino-5-nitrothiazole). The new compounds included 2-nitroimidazole nucleoside analogues, nitrotriazoles and other nitroaromatics, non-nitro compounds, and electron-affinic compounds that readily intercalate DNA. The sensitizing activity in the EMT6 single cells correlated not only with the reduction potential but, for some compounds, also with the reactivity with non-protein sulphydryls. The sensitizers were also tested using the EMT6 spheroids and solid tumours. The patterns of changes in sensitizer enhancement ratios (SERs) for single cells, spheroids, and solid tumours were classified into two types: (1) SERs for the three testing systems were similar; and (2) SERs decreased in the order of: single cells, spheroids, and solid tumours. Only nitroimidazole and nitrotriazole derivatives belonged to the former type. RK-28 and RK-29, 2-nitroimidazoles with sugar analogue components, had in vivo effects almost equal to those of MISO. Also 3- and 4-nitrotriazole derivatives had definite in vivo effects.
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2-硝基咪唑核苷 (RA-263) 的放射增敏、药代动力学和毒性。
影响因子：
3.4
作者：
Agrawal,KC;Rupp,WD;Rockwell,S
通讯作者：
Rockwell,S
影响因子：
7.3
作者：
Sakaguchi,M;Larroquette,CA;Agrawal,KC
通讯作者：
Agrawal,KC
邻位取代的 4- 和 5-硝基咪唑的放射增敏和细胞毒性特性：NPSH 反应性的作用。
DOI：
10.1016/0360-3016(82)90649-6
发表时间：
1982
期刊：
International journal of radiation oncology, biology, physics
影响因子：
--
作者：
Astor,M;Hall,EJ;Martin,J;Flynn,M;Biaglow,J;Parham,JC
通讯作者：
Parham,JC
SR-2508：2-硝基咪唑酰胺，临床使用的放射增敏剂应优于米索硝唑。
DOI：
10.1016/0360-3016(81)90460-0
发表时间：
1981
期刊：
International journal of radiation oncology, biology, physics
影响因子：
--
作者：
Brown,JM;Yu,NY;Brown,DM;Lee,WW
通讯作者：
Lee,WW
谷胱甘肽在米索硝唑缺氧细胞细胞毒性中的作用。
影响因子：
11.2
作者：
Bump,EA;Taylor,YC;Brown,JM
通讯作者：
Brown,JM