Nagao Y, Sano S, Ochiai M, Fuji K, Nishimoto S, Kagiya T, Murayama C, Mori T, Shibamoto Y, Sasai K
Chem Pharm Bull (Tokyo). 1989 Jul;37(7):1951-3. doi: 10.1248/cpb.37.1951.
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).
为了开发用于放射治疗的低氧癌细胞新型放射增敏剂,合成了3-硝基-1,2,4-三唑(3-NTR)的新区域异构体衍生物4a-f和5a-f。N(2)-取代的3-NTR衍生物5a-f在体外(中国仓鼠V79细胞)对低氧细胞的放射增敏作用比N(1)-取代的3-NTR衍生物4a-f更强,但在体内(接种到C3H/He小鼠体内的SCCVII癌细胞)则较弱。