A 2-nitroimidazole derivative of the formula:
wherein Rf is a group of the following formula (II) or (III):
-CH₂CFXCH₂OR₁ (II)
wherein X is a hydrogen atom or a halogen atom; R₁ is a group of the formula:
-CH(CH₂OR₂)₂
-(CH₂)ℓOR₂
-(CH₂)ℓCOR₂ or
wherein R₂ is a hydrogen atom, a hydroxyl group, a C₁-C₃ alkyl group, a C₂-C₄ acyl group, benzylidene or acetonide; R₃ is a hydrogen atom or a C₁-C₃ alkyl group; Z is a hydrogen atom, COOY, COOR3, CONHOY, CONR₄R₅ (wherein R₄ and R₅ are hydroxyl group-containing C₁-C₃ alkyl groups or hydrogen atoms; Y is a hydrogen atom or a monovalent metal atom), an amino group, a hydroxyl group or OR₃; ℓ is an integer of 1 to 3; o is an integer of 0 to 3; p is an integer of 0 to 2; q is an integer of 0 to 3; m and n are integers of 0 to 4; and 1 ≦ m + n ≦ 4
or
wherein R₃, X and p are the same as defined above; Z′ is the same as Z or is OCOOCH₃; r is an integer of 1 to 3; s is 0 or 1; t is an integer of 0 to 4 provided that when p = 0, s ≠ 0 and at least one X is a fluorine atom; and a radiosensitizer comprising said nitroimidazole derivative.
式中的
2-硝基咪唑衍
生物:
其中 Rf 为下式(II)或(III)的基团:
-CH₂CFXCH₂OR₁ (II)
其中 X 是氢原子或卤素原子;R₁ 是下式中的基团:
-CH(CH₂OR₂)₂
-(CH₂)ℓOR₂
-(CH₂)ℓCOR₂或
其中 R₂ 是氢原子、羟基、C₁-C₃ 烷基、C₂-C₄酰基、亚苄基或
丙酮;R₃ 是氢原子或 C₁-C₃ 烷基;Z 是氢原子、COOY、COOR3、CONHOY、CONR₄R₅(其中 R₄ 和 R₅ 是含羟基的 C₁-C₃ 烷基或氢原子;Y 是氢原子或一价
金属原子)、
氨基、羟基或 OR₃; ℓ 是 1 至 3 的整数; o 是 0 至 3 的整数; p 是 0 至 2 的整数; q 是 0 至 3 的整数; m 和 n 是 0 至 4 的整数;且 1 ≦ m + n ≦ 4
或
其中R₃、X和p与上文所定义的相同;Z′与Z相同或为OCOOCH₃;r为1至3的整数;s为0或1;t为0至4的整数,条件是当p=0时,s≠0,且至少一个X为
氟原子;以及包含所述硝基
咪唑衍
生物的放射增敏剂。