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Hypoxic cell sensitization to radiation damage by a new radiosensitizer: cis-dichloro-bis(1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole-N3)platinum(II) (flap).一种新型放射增敏剂对缺氧细胞辐射损伤的增敏作用：顺式二氯 - 双（1 - （2 - 羟乙基）- 2 - 甲基 - 5 - 硝基咪唑 - N3）铂（II）（弗拉普）
Br J Cancer. 1982 Nov;46(5):701-5. doi: 10.1038/bjc.1982.261.
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引用本文的文献

1
Sister chromatid exchanges induced by two radiosensitizing platinum compounds (cis-dichloro-bis isopropylamine trans dihydroxy platinum IV (CHIP) and cis platinum metronidazole2Cl2(FLAP)) in CHO cells in vitro.两种放射增敏铂化合物（顺式二氯双异丙胺反式二羟基铂IV（CHIP）和顺铂甲硝唑2Cl2（FLAP））在体外诱导CHO细胞中的姐妹染色单体交换。
Br J Cancer. 1983 Dec;48(6):803-7. doi: 10.1038/bjc.1983.270.

本文引用的文献

1
Potentiation of the radiation response of hypoxic mammalian cells by cis-dichlorobis(isopropylamine)trans-dihydroxy platinum IV (CHIP).顺二氯双（异丙胺）反二羟基铂（IV）（CHIP）对缺氧哺乳动物细胞辐射反应的增强作用
Br J Radiol. 1981 Jun;54(642):529-30. doi: 10.1259/0007-1285-54-642-529.
2
The response of Chinese hamster (ovary) cells to protracted irradiation from 252Cf and 60Co.中国仓鼠（卵巢）细胞对来自²⁵²Cf和⁶⁰Co的长时间照射的反应。
Br J Radiol. 1973 Nov;46(551):991-5. doi: 10.1259/0007-1285-46-551-991.
3
The selective toxicity of antimicrobial nitroheterocyclic drugs.抗菌硝基杂环药物的选择性毒性。
J Gen Microbiol. 1973 May;76(1):135-45. doi: 10.1099/00221287-76-1-135.
4
The effect of combined treatment with a platinum complex and ionizing radiation on chinese hamster ovary cells in vitro.铂配合物与电离辐射联合处理对体外培养的中国仓鼠卵巢细胞的影响。
Br J Cancer. 1976 Apr;33(4):450-8. doi: 10.1038/bjc.1976.70.
5
The mechanism of action of cis-dichloro-bis (isopropylamine) trans dihydroxyplatinum IV (CHIP) on Chinese hamster and C3H mouse tumor cells and its interaction with X-irradiation.顺二氯双（异丙胺）反二羟基铂（IV）（CHIP）对中国仓鼠和C3H小鼠肿瘤细胞的作用机制及其与X射线照射的相互作用。
Int J Radiat Oncol Biol Phys. 1979 Aug;5(8):1341-4. doi: 10.1016/0360-3016(79)90666-7.
6
Radiation-induced DNA damage and lethality in E. coli as modified by the antitumor agent cis-dichlorodiammineplatinum (II).
Radiat Res. 1977 Aug;71(2):447-60.
7
Peripheral neuropathy related to misonidazole: incidence and pathology.与米索硝唑相关的周围神经病变：发病率与病理学
Br J Cancer Suppl. 1978 Jun;3:271-5.

一种新型放射增敏剂对缺氧细胞辐射损伤的增敏作用：顺式二氯 - 双（1 - （2 - 羟乙基）- 2 - 甲基 - 5 - 硝基咪唑 - N3）铂（II）（弗拉普）

Hypoxic cell sensitization to radiation damage by a new radiosensitizer: cis-dichloro-bis(1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole-N3)platinum(II) (flap).

作者信息

Bales J R, Sadler P J, Coulson C J, Laverick M, Nias A H

出版信息

Br J Cancer. 1982 Nov;46(5):701-5. doi: 10.1038/bjc.1982.261.

DOI:10.1038/bjc.1982.261
PMID:6890846
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2011175/
Abstract

A new, stable platinum coordination complex (FLAP) containing the 5-nitroimidazole, metronidazole, has been prepared and characterized. The square-planar platinum(II) complex has two metronidazole molecules and two chlorine atoms in the cis configuration. The properties of FLAP differ significantly from metronidazole alone or other platinum complexes tested in the same system. It has a low toxicity towards Chinese hamster ovary cells and is a very effective radiosensitizer toward hypoxic cells in vitro: a one-h pretreatment with a non-toxic dose of 50 microM gave an enhancement ratio of 2.4. No potentiation of aerated cells to X-irradiation damage was observed after a similar schedule of pretreatment at the higher dose of 100 microM FLAP.

摘要

一种含有5-硝基咪唑（甲硝唑）的新型稳定铂配位络合物（FLAP）已被制备并表征。该平面正方形铂（II）络合物具有两个处于顺式构型的甲硝唑分子和两个氯原子。FLAP的性质与单独的甲硝唑或在同一系统中测试的其他铂络合物有显著差异。它对中国仓鼠卵巢细胞毒性较低，并且在体外对缺氧细胞是一种非常有效的放射增敏剂：用50微摩尔无毒剂量进行1小时预处理，增强比为2.4。在100微摩尔FLAP较高剂量下进行类似的预处理后，未观察到对有氧细胞X射线辐射损伤有增强作用。