PURPOSE: An antitumor agent having improved cytocidal and antitumor effects, comprising 2,3,6-trichloronaphthazarin, etc., as active ingredients.
CONSTITUTION: An antitumor agent comprising a compound shown by formula I [ring A is group shown by formula II, formula III, formula IV or formula V (numbers 1W4 show positions of substituent groups R1WR4, R1WR3=Cl and R4=H; R1, R2 and R4=Cl and R3=H; R1 and R2=OCH3, R3=Cl and R4=H; R1 and R2=OCH3, R3=H and R4=Cl; R1WR3=OCH3 and R4=H; R1, R2 and R4=OCH3 and R3=H) as an active ingredient. 2,3,6-Trichloronaphthazarin compound having antitumor action wherein ring A in the formula I is group shown by formula II, R1WR3 are Cl and R4 is H is obtained by condensing 2,3- dichloromaleic anhydride with 2,3,6-trichloronaphthazarin in the presence of anhydrous AlCl3 and NaCl under heating. This compound is reacted with CH3ONa to give a compound shown by formula VI and a compound shown by formula VII of the compound shown by formula I, having antitumor action.
BIOCHIM.BIOPHYS.ACTA=1984
CHEM.PHARM.BULL=1977
JOURNAL OF MEDICINAL CHEMISTRY=1983