Synthesis Of Indole Alkaloids-evoaline And Ellipticine And The Biological Activity Of Their Derivatives

Alkaloids are alkaline nitrogenous compounds found in living organisms,which are widely concerned because of their rich physiological activities.Indole alkaloids are the most abundant alkaloids.Evodiamine is derived from the traditional Chinese drug,which has the pharmacological functions of lowering blood pressure,tranquilizing and vomiting,etc.It has been reported to have anti-tumor and anti-alzheimer’s activity in recent years.Ellipticine is extracted from the Ochrosia Elliptica Labill.,O.balansae and O.moorei,which is an alkaloid with a tetracyclic structure has anti-tumor activity.These two kinds of alkaloids have certain similarity in the structure.In this paper,a more simple method was used to synthesize evodiamine and rutecarpine,29 related derivatives were prepared.Artificial synthesis of 7 natural products,including Euxylophoricine C and Euxylophoricine F,was first synthesized.The synthesis procedure of ellipticine was optimized,and the total yield ratio of the route increased to 45%was significantly higher than that of the literatures reported 21%,and 17 related intermediates and derivatives were synthesized,14 of which were new compounds have not been reported.In this paper,the synthetic derivatives were screened in vitro and in vivo activities,and the preliminary structure-activity relationship was summarized.R-23,R-29 of the evodia derivatives which have well anti Alzheimer’s disease activity.E-1,E-11,E-12 of ellipticine derivatives have good in vitro antitumor activity and E-12 showed satisfactory in vivo antitumor activity which provides a good reference for further study.