Radiosensitization in vitro and in vivo by 3-nitrotriazoles
| Autor: | Koichi Sakano, Mitsuyuki Abe, Yuta Shibamoto, Sei-ichi Nishimoto, Tsutomu Kagiya, Ryoji Kimura, Koji Ono, Takehiro Nishidai |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
Cancer Research
Misonidazole Radiation-Sensitizing Agents Triazole Pharmacology In Vitro Techniques Toxicology chemistry.chemical_compound Mice In vivo Cricetinae Medicine Animals Radiology Nuclear Medicine and imaging Cytotoxicity Mice Inbred BALB C Mice Inbred C3H Radiation business.industry Neoplasms Experimental V79 cells Triazoles Nitro Compounds Combined Modality Therapy In vitro Oncology chemistry Nitroimidazoles Toxicity Antineoplastic Drugs Female business Neoplasm Transplantation |
| Zdroj: | International journal of radiation oncology, biology, physics. 12(7) |
| ISSN: | 0360-3016 |
| Popis: | A series of 3-nitro-1,2,4-triazole derivatives bearing various types of side chain (R) at the N1-position (AK-2000 series) were synthesized and their radiosensitizing effect and toxicity in vitro and in vivo were investigated, in comparison with those of Misonidazole (MISO), SR-2508, and RSU-1069. Of the fifteen 3-nitrotriazoles tested, all had sensitizing effects in vitro on hypoxic V79 cells. Also, all but one had definite effects on solid EMT6/KU and SCCVII tumors in vivo. For many of the triazole compounds, the degree of radiosensitization in vitro and in vivo appeared identical. However, they were generally less efficient, both in vitro and in vivo, than the corresponding 2-nitroimidazoles, whereas their aerobic cytotoxicity and toxicity to mice (LD50/7) were comparable to those of the 2-nitroimidazoles. Considering the sensitizing effect and toxicity, AK-2123 (R = CH2CONHC2H4OCH3) may be as useful as MISO, but none of the triazoles have been proved to be superior to SR-2508. |
| Databáze: | OpenAIRE |
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