13556-29-1Relevant articles and documents
Novel anthraquinone derivatives with redox-active functional groups capable of producing free radicals by metabolism: Are free radicals essential for cytotoxicity?
Barasch, Dinorah,Zipori, Omer,Ringel, Israel,Ginsburg, Isaac,Samuni, Amram,Katzhendler, Jehoshua
, p. 597 - 615 (1999)
The mode of action of antitumour anthraquinone derivatives (i.e. mitoxantrone) is not clearly established yet. It includes, among others, intercalation and binding to DNA, bioreduction and aerobic redox cycling. A series of anthraquinone derivatives, with potentially bioreducible groups sited in the side chain, have been synthesized and biologically evaluated. Their redox and cytotoxic activities were screened. Derivatives which bear a 2-(dimethylamino)ethylamino substituent, known to confer high DNA affinity, demonstrated cytotoxicity but not redox activity (beside the anthraquinone reduction). Conversely, derivatives which showed redox activity were not cytotoxic toward the P388 cell line. The results suggest that bioreduction is not the main mode of action in the cytotoxicity of anthraquinones.
Tumour targeting prodrugs activated by metallo matrixproteinases
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Page 7, (2010/02/09)
A-(B)n—X ??(I) A-(B)n-Q ??(II) Numbers in Parentheses denote examples in the specification A compound is of general formula (I) wherein (A) is a moiety comprising one of more of a heterocylcic ring, a carbocyclic ring and a fused ring system, the ring or ring system being essential for a biological activity of the compound by action at a nucleic acid or protein target (B) is a bivalent spacer molecule attached directly to the ring system n is an integer 0 or 1 and (X) is a monovalent moiety containing a amide bond that is cleavable by the action of a matrix metalloproteinase enzyme such as to produce a compound of formula (II) wherein the efficacy of the biological activity of the compound of formula (II) is increased over that of the compound of formula (I).