Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Patent
1996-07-23
1998-05-12
Geist, Gary
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
564163, C07C23365
Patent
active
057507821
ABSTRACT:
The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 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. ##STR1##
REFERENCES:
patent: 5171889 (1992-12-01), Anderson
Palmer et al., "Hypoxia-Selective . . . Cells", J. or Medicinal Chemistry, vol. 35, No. 17, pp. 3214-3222., Aug. 1992.
Denny William Alexander
Palmer Brian Desmond
Wilson William Robert
Cancer Research Campaign - Technology Limited
Geist Gary
Keys Rosalynd A.
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