Study On The Preparation Of Biphenyl Cyclooctadiene Lignan Derivatives And Their Partial Biological Activities

This thesis consists of three chapters.Chapter 1 mainly describes research status and importance of schisandhenol,one of dibenzocycoloctadiene lignans.Chapter 2 is experimental part,containing chemical study(systhesis of schisandhenol derivatives and study of methodology of organic synthesis)and bioactivity test(anti-TMV,anti-bacterial activity,and anti-tumor activity).Chapter 3 is the part of conclusion.Schisandhenol is one of dibenzocycoloctadiene lignans,which shows less bioactivities,only activities of liver-protection and anti-TMV based on former study of our team,comparing with the other dibenzocycoloctadiene lignans.So the continuous study on schisandhenol is of great importance.On the basis of combination principles and other theories for design of new drugs,thirty-three derivatives of dibenzocycoloctadiene lignan(mainly schisandhenol derivatives)were designed and synthesized.Besides,we systematically studied on one new methodology for dehalogenation of aryl halides,which was found in the process of synthesis of derivatives unexpectedly.After completion of synthesis of derivatives,we did bioactivity test of part of derivatives against TMV,bacteria,and tumor cell lines.The outcomes showed that schisandhenol dervatives possess great curative effect activities(At the concentration of 0.15 mM,W-2 shows 78.0±3.8%.At the concentration of 0.25 mM,W-7 shows64.2±9.4%.At the concentration of 0.5 mM,W-16 shows 64.8±6.0%)and protective effect activities(At the concentration of 0.15 mM,W-6 shows 83.6±8.8%.At the concentration of 0.5 mM,W-2 shows 71.5±4.0%)against TMV.The anti-bacterial activity of part of derivatives is low,even the highest inhibitory activity(W-11)is lower than 15%.The anti-tumor activities(A549 and K562 cell lines)of part of dibenzocycoloctadiene lignan derivatives are alsoweak effect.Finally,this thesis was summarized and great importance of which was hoped for future study.