Catalytic Synthesis And Activity Of Carboline Derivatives

Carboline alkaloids are important subfamilies of natural alkaloids.Because of the planar aromatic ring systems,carboline derivatives could easily embedded in DNA,consequently,this group of alkaloids showed interesting antibacterial,antiviral,anti-tumor and inhibition central nervous system and other important biological activitives.In the literature,synthesis of carboline derivatives mostly focused on the formation of the pyridine ring by Pectet-Spengler reaction.Other methods included that synthesis of carboline structures via metal-catalyzed reactions.These methods have obvious drawbacks such as long reaction steps,using harsh reaction conditons.Development of novel and efficient synthesisand investigating the bioactivities of new carboline compounds still remain desirable.In recent years,metal-catalyzed C-H activation has drawn considerable attention.Studies toward construction of the pyridine rings of isoquinoline by C-H activation have also been reported.In this thesis,we reported that synthesis carboline derivatives was accomplished via transition metal-catalyzed C-H activation as key step for construction of the pyridine ring using indoly hydroxamate as starting materiasl.And the reaction is successfully applied for the construction of skeletion of the marine natural product Eudistomin U.Eleven new ?-carboline and ?-carboline derivatives were synthesized by this method,Preliminary bioactivities of these new carbolines was tested.Results show that compunds 123 and 134 have good restraint function to Hela;Compounds 123 and 128 inhibite BGC-823;Compounds 123 and 120 inhibite Hep-2.