Synthesis And Anticancer Activity Of Novel Anthraquinone Derivatives

Anthraquinones is the largest number of all kinds of natural quinones, a class ofcompounds. A long time ago, anthraquinone was used as natural dyes, but later found theyhave a lot of medicinal value. For example, they have anti-bacterial, anti-inflammatory,antiviral, anticancer, protective and choleretic, eyesight, nootropic, anti-aging, anti-mutagenic,anti-UV. Moreover, the anthraquinone has promoting blood circulation, sleep-promotingeffect, lipid-lowering effect and increase immune function and role.Since the1970s, also found a variety of activity dihydroxyanthraquinone derivatives.Found from Sesamum indicum antifungal activity anthrasesamone; reported in the literaturemethoxy daunorubicin(Idarubicin) are parallelism side of the quinone nucleus of a saturatedring glycosidic compounds belonging to the antibiotic class of antineoplastic agents, a widerange of applications in the treatment of leukemia.Hydrazide compounds because of their good biological, pharmacological activity andother aspects of superior perfomance, are potential therapeutic drugs and functional materials,but studies have shown that the presence of–NH2biobody has a certain toxicity. By thecondensation of aldehydes or ketones and hydrazide hydrazone compounds both thecontinuation of their excellent activity can be effective in reducing the toxcity, and thereforereceived extensive attention in recent years. Thiourea because of the superiority of thebiological, pharmacological activity and other aspects of energy, it is a research anddevelopment of its value.The group has been working on the the structure of anthracyclines structure modificationand transformation in order to obtain better anti-tumor actvity and lower toxcity of newanthracyclines. Based on this, we use the principle of the active fragment of mosaic synthesis of a new anthraquinone compounds, and further screened for their biological activity. Themain contents of this study include:1. Synthesis of2-(1,4-dihydroxy-9,10-anthraquinone-2-yl)methylene acylhydrazonederivatives.1,4-dihydroxy-9,10-anthraquinone as raw material, the use of three-step one-potmethod to synthesize1,4-dihydroxy-2-formyl-9,10-anthraquinone. By the condensation of1,4-dihydroxy-2-formyl-9,10-anthraquinone and hydrazide to obtain acylhydrazonecompounds.2. Synthesis of2-(1,4-dihydroxy-9,10-anthraquinone-2-yl)methylene thiosemicarbazidederivatives. The same method to the synthesis of1,4-dihydroxy-2-formyl-9,10-anthraquinone,and then the condensation reaction with thiosemicarbazide, a series of2-(1,4-dihydroxy-9,10-anthraquinone-2-yl)methylene thiosemicarbazide derivatives.