Synthesis Of Podophyllotoxin Derivatives As Anti-cancer Agents And Its Activity

Podophyllotoxin is a bioactive lignan isolated from Podophyllum peltatum L., P. emodi W., or P. Pleianthum H. It was firstly used as a poison and later for treatment of various pathogenic infections and venereal warts. Then people found its antitiumur activity. But because of its toxicity, people began to reform its structure for safely clinic use. Over a period of about 20 years till the discovery of VP-16 and VM-26, which are currently used in front-line cancer chemotherapy against various cancers including small cell lung cancer, testicular carcinoma, and lymphoma. Their therapeutic use has encountered certain limitations such as acquired drug resistance and poor water solubility. To overcome such problems, extensive synthetic efforts have been carried out by a number of researchers.Acylhydrazones as special schiff base, have strong coordination ability, good biological activities and other excellent properties, which make them to be potential drugs and functional materials and have become the focus of research in pesticides and medicines. In recent years, scientists have paid more attention to these compounds.In this paper, about 20 podophyllotoxin derivatives with the D-ring lactone opened were synthesized in two steps from podophyllotoxin and evaluated as antitumur agents in vitro. Most of the derivatives exhibit antitumur activity. All the target compounds are all characterized by MS and 1H-NMR.