Modification Of 16-Dehydropregnenolone Acetate And Research Of Anti-Tumor Bioactiviteis

16-Dehydropregnenolone Acetate (16-DPA) is the intermediate of steroid hormone and produced from saponins. 16-DPA can be synthesize hormonal drugs, such as Cortisone, Prednisone, Topsyne, Dexamethasone, which take good effect on glycometabolism, anti-inflammatory, antiviral, antishock, antianaphylaxis and immunological disease.In this thesis, the raw material, 16-DPA, firstly reacts with hydroxylamine hydrochloride, intermediate oxime obtained. Then the oxime reacted with a range of acyl chloride, twenty-four compounds LG-1~LG-24 were synthesized.The oxime is also reduced to amine by sodium in the alcohol, then the amine reacted with a range of acyl chloride, and eight compounds LG-26~LG-33 were obtained. All compounds were identified by nuclear magnetic resonance spectroscopy, infrared, optical rotation and mass spectrometry.All compounds synthesized took cytotoxicity assay on leukemia cell line NB4, prostatic cancer cell line PC-3 and cervical carcinoma cell line Hela. As a result, the compound LG-26 showed significant activity on NB4 at 30μmol/L. The death rate was 52% after 24 hours while 71.2% after 48 hours. the compound LG-A showed significant inhibitory activity against PC-3 at 1μmol/L. The death rate was 52.2% after 24 hours while 83% after 48 hours. The compound LG-A showed significant activity on Hela at 1μmol/L. The death rate was 54.2% after 24 hours while 89% after 48 hours. The rest compounds have different cytotoxicities against on NB4, PC-3 and HELA.