Synthesis And Antitumor Activity Of Schiff Bases Of Indolocarbazole Compounds

Indole carbazole compounds are extracted from the fermented liquid of a natural alkaloid of S treptomyces staurosoreus.Indole carbazole derivatives have obvious antitumor activity,anti hyperten sion and antibacterial so on.Some of these compounds have entered the stage of anti-cancer drugs clinical research,hoped to become a new cancer drugs in the future.Scientific research workers tr y to modify maleic imide ring N so that they can increase the anticancer activity.Through ringing into different substituent on N of maleic imide,we can get a variety of indole carbazole derivativ es.Thiocarbamide and Acyl hydrazone compounds have high biological activity.Therefore,wedesi gn that with the indole carbazole heterocyclic combination of thiocarbamide compounds and acyl h ydrazone compounds to preparae new antitumor activity of indole carbazole compounds.In the thesis,we use the principle of the active fragment of mosaic synthesis of two kinds(four series)compounds,and further screened for their biological activity.The results show that most of the compounds have high inhibitory activity cyclin CDC 25 B,so they have potential anti-cancer activity.1.Synthesis of new type of double indole maleic imide acyl hydrazone and thiocarbamide.2,3-dichloro maleic anhydride as starting materials,using 2,3-dichloro-N-methyl maleic imide and in dole grignard reagent reaction obtain 2,3-2(3-indole)-N-methyl maleic imide,after tworeactions to get 1-amino-3,4-2(3-indole)-3-pyrrole Lin-2,5-diketone compound,then reaction with aldehyde and isothiocyanates compounds,new type of double indole maleic imide acyl hydrazone and thiocarba mide were obtained at last.2.In order to explore the change of biological activity of the reaction of rigid indole carbazo le ring with acyl hydrazone and thiosemicarbazide compounds.Through cyclization,We get 6-meth yl-indole[2,3-a]pyrrole[3,4-c]carbazole-5,7-diketone compound.After a series of reactions to get 6-amino-indole[2,3-a] pyrrole[3,4-c]carbazole-5,7-diketone compound.Then reaction with aldehyde and isothiocyanates compounds,the corresponding acyl hydrazone compounds and thiocarbamide co mpounds were obtained at last.