Radiosensitization in vitro and in vivo by 3-nitrotriazoles
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 = CH/sub 2/CONHC/sub 2/H/sub 4/OCH/sub 3/) may be as useful as MISO, but none of the triazoles have been proved to be superior to SR-2508.
- Research Organization:
- Kyoto Univ., Japan
- OSTI ID:
- 5004556
- Journal Information:
- Int. J. Radiat. Oncol., Biol. Phys.; (United States), Vol. 7
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
NITRO COMPOUNDS
RADIOSENSITIVITY EFFECTS
TOXICITY
TRIAZOLES
ANOXIA
HAMSTERS
IN VITRO
IN VIVO
MICE
MISONIDAZOLE
NEOPLASMS
RADIOSENSITIZERS
ANIMALS
ANTINEOPLASTIC DRUGS
AZOLES
DISEASES
DRUGS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
MAMMALS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RODENTS
VERTEBRATES
560152* - Radiation Effects on Animals- Animals
560305 - Chemicals Metabolism & Toxicology- Vertebrates- (-1987)