Nitrobenzyl mustard quaternary salts and their use as hypoxia-se

Details Nitrobenzyl mustard quaternary salts and their use as hypoxia-se Nitrobenzyl mustard quaternary salts and their use as hypoxia-se

1997-07-31

1999-02-16

Davis, Zinna Northington

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514311, 514365, 514427, 514438, 514643, 546139, 546176, 548561, 548205, 549 74, 564281, A61K 3114, A61K 3138, A61K 3140, C07C21163

Patent

active

058721290

ABSTRACT:
##STR1## Nitrobenzyl mustard quaternary salts of formula (I), and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.3 -- or CR.sub.1 .dbd.CR.sub.2 -- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionally substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or ether groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH-- replared by --N.dbd.); with the proviso that when Y=Cl or Br, Q=Me, and X=--CH.sub.2 -- then Ar.noteq.2-nitrophanyl or 4-nitrophenyl.

REFERENCES:
patent: 3935182 (1976-01-01), Jefferies et al.
patent: 4206144 (1980-06-01), Jefferies et al.
R. Bruni et al., "Potential carcinolytic agents. VI. New deactivated biological alkylating agents", Experientia, vol. 24, No. 4, 1968, p. 325.
F. Copp et al., "Phosphorylated quaternary ammonium compounds of improved oral absorption", Chemical Abstracts, vol. 61, Abstract No. 9435a, 1964.
M. Tercel et al., "Nitrobenzyl mustard quaternary salts: A new class of hypoxia-selective cytotoxins showing very high in vitro selectivity", J. Med. Chem., vol. 36, No. 17, 1993, pp. 2578-2579.

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