Radiosensitizing hypoxic cells with new 3-nitro-1,2,4-triazole derivatives in vitro and in vivo.
The new regioisomer derivatives 4a-f and 5a-f of 3-nitro-1,2,4-triazole (3-NTR) were synthesized for the development of new radiosensitizers of hypoxic cancer cells for radiotherapy. N(2)-Substituted 3-NTR derivatives 5a-f were stronger radiosensitizers of hypoxic cells in vitro (Chinese hamster V79 cells) than N(1)-substituted 3-NTR derivatives 4a-f, but in vivo they were weaker (SCCVII carcinoma cells inoculated into C3H/He mouse).
Nagao
Y
Y
Sano
S
S
Ochiai
M
M
Fuji
K
K
Nishimoto
S
S
Kagiya
T
T
Murayama
C
C
Mori
T
T
Shibamoto
Y
Y
Sasai
K
K
D000818:Animals; D015687:Cell Hypoxia / Q000187:drug effects*; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002621:Chemistry; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000494:pharmacology; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D009574:Nitro Compounds; D010879:Piperazines; D010880:Piperidines; D011759:Pyrrolidines; D011838:Radiation-Sensitizing Agents; D014230:Triazoles