| abstract |
The invention provides nitroaniline derivatives represented by general formula (I) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO2, CN, COOR1, CONR1R2, CSNR1R2 or SO2NR1R2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH2CH2halogen)2 or N(CH2CH2OSO2R3)2 substituted at any one of the available benzene positions; and where R1, R2 and R3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, in-cluding cyclic structures, or R1 and R2 together with the nitrogen form a heterocyclic structure, and pharmaceutical prepara-tions containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. |