Synthesis And Atitumor Activity In Vitro Of 8-(1-Hydroxyalkyl)-4, 5-Dimethoxy-9, 10-Anthraquinone-1-Car-Barbaldehyde

The tumor is still to endanger the most familiar and the most serious disease of mankind's life in the world nowadays.Anthraquinones showed significant antitumor activity.However,their strong toxicity side effect and multidru9 resistance limit the application in clinical.Based on enhance antitumor activity,decrease toxicity side effect and comprehensive study on the antitumor mechanism and structure-activity relationships,as 1,8-dihydroxy-9,10-anthraqunone starting material it was methylated and via reduction reaction to produce 1,8-dimethoxyanthracene.and was formylated with phosphoryl trichloride obtained 4,5-dimethoxyanthracene-1,8-dicarbaldehyde.8-formyl group reacted with varies alkylbromomagnesium(Grignard reagents) to form 8-(1-hydroxyalkyl) -4,5-dimethoxy-9,10-dioxoanthracene-1-carbaldehyde.it partially was oxydated to produce 8-(1-hydroxyalkyl)-4,5-dimethoxy-9,10-anthraqunone-1-carbaldehyde.All of the 16 target componds couldn't searched in literatures.The antitumor activity tests in vitro of the above compounds were carried on P388 mice leukaemia cells.The results showed antitumor activity on P388 mice leukaemia cells of 4,5-dimethoxyanthracene-1,8-dicarbaldehyde and 8-(1-hydroxyalky 1)-4,5-dimethoxyanthracene-1-carbaldehyde could not be ovserved in vitro experiment. However,most of 8-(1-hydroxyalkyl)-4,5-dimethoxy-9,10-anthraquinone-1-carbaldehy de showed significant antitumor activity against P388 cells.The introduction of hydroxyalkyl chain to anthraquinone structure cytotoxicity was increased,and alkyl chain length at C2-C6 showed higher.When the elongation of alkyl group lover 6 carbon atoms the cytotoxicity decreased.The common effect of anthraquinone nucleus and suitable hydroalkyl chain length could affect favorable cytotoxicity.However,anthracene nucleus,hydroalkyl chain,even if their common effect couldn't.