| Li Wuling,Yang Xinhai.A biological evaluation on in vitro radiosensitization of nitrotriazole derivatives[J].Chinese Journal of Radiological Medicine and Protection,1997,17(5):324-327 |
| A biological evaluation on in vitro radiosensitization of nitrotriazole derivatives |
| Received:June 11, 1996 Revised:December 19, 1996 |
| DOI： |
| KeyWords:Radiosensitization Nitrotriazole derivatives |
| FundProject:国家自然科学基金 |
| Author Name | Affiliation | | Li Wuling | Beijing Medical University, Beijing 100083, China | | Yang Xinhai | Beijing Medical University, Beijing 100083, China | | 赵毅强 | Beijing Medical University, Beijing 100083, China | | 沈磊 | Beijing Medical University, Beijing 100083, China | | 蔡松君 | Beijing Medical University, Beijing 100083, China | | 路新华 | Beijing Medical University, Beijing 100083, China |
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| Abstract:: |
| Objective To assess the radiosensitization of nitrotriazole derivatives and elucidate the structure activity relationships within this group of compounds. Method The partition coefficient (p), reduction potential (E1/2),cytotoxicity and sensitization activity were determined by HPLC, polarography and colony formation, respectively. Results It was found that among these 22 derivatives,two compounds were more efficient than MISO,and other three were of the same efficiency as MISO was in radiosensitizing hypoxic cells,the rest showed poor radiosensitizing properties.As 2-nitroimidazoles,the radiosensitizing activity of a 3-nitrotriazole derivative correlates with its electron affinity,determined as E1/2,half wave reduction potential.The greater is the electron affinity i.e.the more positive the E1/2,the greater is the radiosensitizing efficiency.The value of E1/2,partition coefficient p value and cytotoxicity of a nitrotriazole derivative are influenced by the structure and chemical properties of the substituent at N1 or 5 position of triazole ring.The nitrotriazoles examined show only limited defferential hypoxic:aerobic toxicity. Conclusion Although the nitrotriazole derivative are not viable hypoxia-mediated cytotoxins, the radiosensitization of some of them should be studied thoroughly. |
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