NITROANILINE DERIVATIVES AND THEIR USE AS ANTI-TUMOR ACTIVE SUBSTANCES

摘要

PCT No. PCT/GB92/02199 Sec. 371 Date May 26, 1994 Sec. 102(e) Date May 26, 1994 PCT Filed Nov. 27, 1992 PCT Pub. No. WO93/11099 PCT Pub. Date Jun. 10, 1993 IMAGE (I) 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, including cyclic structures, or R1 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.