Studies On The Syntheses And Anti-tumor Activity Of Andrographolide Derivatives

In this thesis, mounts of literatures on andrographolide were cited, basing on which some of derivatives of andrographolide have been designed and synthesized with andrographolide as materials . All of them have been tested for anti-tumor activity in vitro and some compounds show good anti-tumor activity. And the relationship of their structure and bioactivity have been discussed. The synthesis of compound 4 which show a good activity for anti-inflammatory in vivo and solubility in waterwas optimized. The works are as followings:1. A series of derivatives of cyclophosphate andrographolide have been designed and synthesized with andrographolide as materials through intermediate 14-deoxyandrographo lide, and their structures have been identified by elemental analysis, IR, MS, NMR et al.2. The corresponding cyclophasphate derivatives of them were synthesized by the same way with the 1,2-isopropyloxylfuringlucose and 1,2-isopropyloxylfurinxylose as the materials. The findings of research show the distinct of the shifts in the 31P-NMR between pentacyclo and hexcyclophasphate.for anti-inflammatory in vivo and solubility in water, has been synthesized with andrographolide as materials through intermediate 14-deoxyandrographolide in .one pot in a yield of 80%.4. With andrographolide and 14-deoxyandrographolide as materials, others of andrograp -holide derivatives such as 3,19-isopropyloxy 14-deoxyandrographolide, 3,19-isopropyl -oxy andrographolide, 3,19-acetate 14-deoxyandrographolide and so on were synthesized and characterized by spectral analysis. All of them were tested for anti-tumor activity, some of which show good anti-tumor activity.