145-49-3Relevant articles and documents
ANTHARQUINONE COMPOUNDS AS ANTI CANCER COMPOUNDS
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Page/Page column 18-19, (2008/06/13)
Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, -NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.
Process for the manufacture of aminohydroxyanthraquinones
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, (2008/06/13)
The invention relates to a process for the manufacture of an aminohydroxyanthraquinone of the formula STR1 wherein both of X are hydrogen or one X is --NH2 and the other is --OH and Z is hydrogen, C1 -C4 alkyl or carboxyl, with the proviso that, if Z is C1 -C4 alkyl or carboxyl, both of X must be hydrogen, which process comprises reacting a nitroanthraquinone of the formula STR2 wherein both of Y are hydrogen or one Y is --NO2 and the other is hydrogen and Z is as defined for formula (1), with the proviso that, if Z is C1 -C4 alkyl or carboxyl, both of Y must be hydrogen, in an aprotic dipolar solvent, with an alkali metal azide or alkaline earth metal azide, in the temperature range between 0° and 30° C. The reaction products are disperse dyes or intermediates for obtaining vat dyes and disperse dyes.