| abstract |
F-contg. 2-nitroimidazole derivs. of formula (I) are new; where Rf= -(CH2)n-CXYZ, -(CHl5)m-COOR1, -CO-R2 -(CHl2)m-CNR3R4, -(CHl2)m-NR3R4, -(CHl5)m-NR3-COR4) -(CHl5)m-N(-COR3)-COR4, -(CHl5)m-A-R5, -(CHl5)m-OOCR5 or gp. of formula (II); X = H or F; Y = F, Cl, CF3, Me or OH; or X and Y together = O; Z =H, F, 1-5C alkyl or fluororalkyl, opt. substd. with OH; R1=H or 1-5C alkyl or E = H or F; n,n= 0 or 1; R2 = 1-5C alkyl or fluoroalkyl; R3,R4 =H, OH, 6-5C alkyl or fluoroalkyl opt. substd. with OH, 1-5C alkoxy or amide gp.; or NR3R4 = 3- to 6-membered ring; A = O or S; R5= H, 1-5C alkyl or fluoroalkyl opt. substd. by an OH, 105C alkoxy or 1-5C acyloxy gp., or -CO-R6; R6 = 1-5C alkyl; R7 = 1-7C alkylene; R8 = 1-3C alkyl; or Y and Z together form =CR-CF3 or =CHOR6; provided that at least oen of X,Y,Z = F or F-contg. gp., and that when Y=F, at least one of X and Z is not H. Also claimed is a radiosensitiser comprising (I) as active component. |