1,3-Dihydroxy-9,10-anthraquinone衍生物的合成及其藥理活性的探討

Apoptosis causes cell died for a mechanism of the balance of the human tissue growth, and compound that has the activity of the apoptosis may be developed as more specific anticancer agent. In some plants, natural anthraquinone isolated from plants and some synthetic 1,3- dihydroxyanthraquinones showed cytotoxicity due to apotosis. For a continual study on the cytotoxicities and antiplatelet effects of 1,3- dihydroxyanthraquinone derivates, we further synthesized 12 anthraquinone derivatives. 1,3-dihydroxy-4-prenyl-9,10-anthraquinone (5)、3,4-(2,2-dimethylpyrano)-1-hydroxy-9,10-anthraquinone (6)、1-hydroxy-3-prenyloxy-9,10-anthraquinone (7)、3-allyloxy-1-hydroxy- 9,10-anthraquinone (8)、1,3-diallyloxy-9,10-anthraquinone (9)、3-(but-2- enyloxy)-1-hydroxy-9,10-anthraquinone (10)、1,3-bis(but-2-enyloxy)- 9,10-anthraquinone (11)、1-hydroxy-3- acetoxy-9,10-anthraquinone (12)、1-hydroxy-3-propoxy-9,10-anthraquinone (13)、1-hydroxy-3- [3-(isopropylamino)-propoxy]-9,10-anthraquinone (15)、1-hydroxy-3- [3-(tert-butylamino)-propoxy]-9,10-anthraquinone (16) and 1-hydroxy- 3-[3-(n-butylamino)-propoxy]-9,10-anthraquinone (17). Compound 5 showed potent cytoxic effect against several human cancer cell line. 1,3-Dihydroxyanthraquinone with 3-aminopropoxyl side chain showed potent antiplatelet effects.