Design,Synthesis,Biological Activity And Structure-activity Relationship Studies Of Natural Product Cytisine

Tumor is a serious threat to human health.At present,the mechanism of action of anti-tumor drugs and the targets of drugs are diverse,and treatment failure often leads to multi-drug resistance due to tumor cells.Finding safe and effective anti-tumor drugs with small toxicity and side effects has always been the goal of cancer drug developers.Natural products are an important source of drugs and drug lead compounds,and the lead compounds are an important way to obtain new drug candidate compounds and new drugs.The natural product cytisine is a quinolicidine alkaloid derived from seeds of the genus fabaceae and has strong antitumor activity.In this paper,using cytisine as the lead compound,designed and synthesized the cytisine derivatives 1-30,1-20,cytisine derivatives containing acyl structures 1-12,the structures of all the compounds were confirmed by ¹HNMR,¹³CNMR,and high-resolution mass spectrometry,And investigated the new compounds for their anticancer activity,using the lung cancer A549 cells.The test results indicated that all the compounds exhibited inhibitory activity against A549 cells,Introduction of different substituent groups exhibited different inhibitory activities.Of which compounds 5,6,and 7 showed better inhibitory activity,of 51.3%,54.9%,and62.2%,respectively,the activity was higher than the parent compound（37.3%）.Through the research of this paper,it initially provides a theoretical basis for the application of golden sparrow cytisine derivatives in anticancer cancer,and better promotes the medical research and development of lung cancer.