| 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, COOR?1, CONR1R2, CSNR1R2¿ or SO¿2NR?1R2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH¿2?CH2halogen)2 or N(CH2CH2OSO2R?3)¿2 substituted at any one of the available benzene positions; and where R?1, R2 and R3¿ separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R?1 and R2¿ together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. |