5-GLYCOSYLOXY-6-HYDROXYNAPHTHO 2,3-f QUINOLINE-7,12-DIONE HAVING ANTICANCER ACTIVITIES

摘要

As novel compounds which exhibit reduced toxicities but enhanced anticancer activities in comparison with those of known carcinostatic anthracycline derivatives, there is provided a compound of general formula (I) <CHEM> wherein A is methyl group or CF3 group, and B is hydrogen atom, or an electron-withdrawing group chosen from halogeno group and others, provided that B stands for hydrogen atom when A is CF3 and that B stands for an electron-withdrawing group when A is methyl group, and R<1> and R<2> each are hydroxyl group, amino group or an acyloxy group or an aminoalkanoyloxy group, and others, or a pharmaceutically acceptable salt thereof. The compound of general formula (I) possesses activities inhibitory to proliferation of various human cancer cells and is of lower toxicity than that of adriamycin. Further, there is provided, as novel and water-soluble carcinostatic compounds, a compound of general formula (V) <CHEM> wherein A and B have the same meanings as defined above, and R<5> is hydrogen atom or an omega -amino acid residue, and R<6> and R<7> have the same meanings as defined for R<5>, provided that R<5>, R<6> and R<7> do not represent hydrogen atom, simultaneously.